Strategies for Structural Modification of Small Molecules to Improve Blood–Brain Barrier Penetration: A Recent Perspective

Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings

Lipinski, C. A., Lombardo, F., Dominy, B. W., & Feeney, P. J. (1997) · Advanced Drug Delivery Reviews · doi:10.1016/s0169-409x(96)00423-1 · Cited by 11,484

Global, regional, and national burden of neurological disorders, 1990-2016: a systematic analysis for the Global Burden of Disease Study 2016

Feigin, V. L., Nichols, E., Alam, T., Bannick, M. S., Beghi, E., Blake, N., Culpepper, W. J., Dorsey, E. R., Elbaz, A., Ellenbogen, R. G., et al. (2019) · The Lancet Neurology · doi:10.1016/s1474-4422(18)30499-x · Cited by 5,644

Drug-like properties and the causes of poor solubility and poor permeability

Lipinski, C. A. (2000) · Journal of Pharmacological and Toxicological Methods · doi:10.1016/s1056-8719(00)00107-6 · Cited by 3,776

Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings

Lipinski, C. A., Lombardo, F., Dominy, B. W., & Feeney, P. J. (2012) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2012.09.019 · Cited by 3,720

Applications of Fluorine in Medicinal Chemistry

Gillis, E. P., Eastman, K. J., Hill, M. D., Donnelly, D. J., & Meanwell, N. A. (2015) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5b00258 · Cited by 3,692

Fast Calculation of Molecular Polar Surface Area as a Sum of Fragment-Based Contributions and Its Application to the Prediction of Drug Transport Properties

Ertl, P., Rohde, B., & Selzer, P. M. (2000) · Journal of Medicinal Chemistry · doi:10.1021/jm000942e · Cited by 3,149

2019 Alzheimer’s disease facts and figures.

Alzheimer's Association (2019) · Alzheimer's & Dementia · doi:10.1016/j.jalz.2019.01.010 · Cited by 2,461

The blood–brain barrier and blood–tumour barrier in brain tumours and metastases

Arvanitis, C., Ferraro, G. B., & Jain, R. K. (2019) · Nature reviews. Cancer · doi:10.1038/s41568-019-0205-x · Cited by 1,919

Medicinal chemical properties of successful central nervous system drugs

Pajouhesh, H., & Lenz, G. R. (2005) · NeuroRx · doi:10.1602/neurorx.2.4.541 · Cited by 1,608

Physicochemical High Throughput Screening: Parallel Artificial Membrane Permeation Assay in the Description of Passive Absorption Processes

Kansy, M., Senner, F., & Gubernator, K. (1998) · Journal of Medicinal Chemistry · doi:10.1021/jm970530e · Cited by 1,304

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Wager, T. T., Hou, X., Verhoest, P. R., & Villalobos, A. (2010) · ACS Chemical Neuroscience · doi:10.1021/cn100008c · Cited by 1,131

Functional morphology of the blood–brain barrier in health and disease

Liebner, S., Dijkhuizen, R. M., Reiss, Y., Plate, K. H., Agalliu, D., & Constantin, G. (2018) · Acta Neuropathologica · doi:10.1007/s00401-018-1815-1 · Cited by 872

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Yang, C., Hawkins, K. E., Doré, S., & Candelario-Jalil, E. (2019) · American Journal of Physiology-Cell Physiology · doi:10.1152/ajpcell.00136.2018 · Cited by 871

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Crowe, T. P., Greenlee, M. H. W., Kanthasamy, A. G., & Hsu, W. H. (2018) · Life Sciences · doi:10.1016/j.lfs.2017.12.025 · Cited by 721

Structure−Brain Exposure Relationships

Hitchcock, S. A., & Pennington, L. D. (2006) · Journal of Medicinal Chemistry · doi:10.1021/jm060642i · Cited by 716

Central nervous system multiparameter optimization desirability: Application in drug discovery

Wager, T. T., Hou, X., Verhoest, P. R., & Villalobos, A. (2016) · ACS Chemical Neuroscience · doi:10.1021/acschemneuro.6b00029 · Cited by 653

The blood-brain barrier: Physiology and strategies for drug delivery

Pandit, R., Chen, L., & Götz, J. (2020) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2019.11.009 · Cited by 651

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Agrawal, M., Saraf, S., Saraf, S., Antimisiaris, S. G., Chougule, M. B., Shoyele, S. A., & Alexander, A. (2018) · Journal of Controlled Release · doi:10.1016/j.jconrel.2018.05.011 · Cited by 630

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Tang, W., Fan, W., Lau, J., Deng, L., Shen, Z., & Chen, X. S. (2019) · Chemical Society Reviews · doi:10.1039/c8cs00805a · Cited by 610

CNS Drug Design: Balancing Physicochemical Properties for Optimal Brain Exposure

Ranković, Z. (2014) · Journal of Medicinal Chemistry · doi:10.1021/jm501535r · Cited by 592

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Waterbeemd, H. V. D., Camenisch, G., Folkers, G., Chrétien, J. R., & Raevsky, O. A. (1998) · Journal of drug targeting · doi:10.3109/10611869808997889 · Cited by 587

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Wang, Y. I., Abaci, H. E., & Shuler, M. L. (2016) · Biotechnology and Bioengineering · doi:10.1002/bit.26045 · Cited by 572

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Pulgar, V. M. (2019) · Frontiers in Neuroscience · doi:10.3389/fnins.2018.01019 · Cited by 482

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Ghose, A. K., Herbertz, T., Hudkins, R. L., Dorsey, B. D., & Mallamo, J. P. (2011) · ACS Chemical Neuroscience · doi:10.1021/cn200100h · Cited by 463

Aggregated Tau activates NLRP3–ASC inflammasome exacerbating exogenously seeded and non-exogenously seeded Tau pathology in vivo

Stancu, I.-C., Cremers, N., Vanrusselt, H., Couturier, J., Vanoosthuyse, A., Kessels, S., Lodder, C., Brône, B., Huaux, F., Octave, J.-N., et al. (2019) · Acta Neuropathologica · doi:10.1007/s00401-018-01957-y · Cited by 447

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Patel, M. M., & Patel, B. M. (2017) · CNS Drugs · doi:10.1007/s40263-016-0405-9 · Cited by 430

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Erdő, F., Denes, L., & de Lange, E. (2017) · Journal of Cerebral Blood Flow & Metabolism · doi:10.1177/0271678x16679420 · Cited by 426

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Pardridge, W. M. (2020) · Frontiers in Aging Neuroscience · doi:10.3389/fnagi.2019.00373 · Cited by 405

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Khan, A. R., Liu, M., Khan, M. W., & Zhai, G. (2017) · Journal of Controlled Release · doi:10.1016/j.jconrel.2017.09.001 · Cited by 402

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Erickson, M. A., & Banks, W. A. (2018) · Pharmacological Reviews · doi:10.1124/pr.117.014647 · Cited by 398

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Agrawal, M., Ajazuddin, Tripathi, D. K., Saraf, S., Saraf, S., Antimisiaris, S. G., Mourtas, S., Hammarlund-Udenaes, M., & Alexander, A. (2017) · Journal of Controlled Release · doi:10.1016/j.jconrel.2017.05.019 · Cited by 356

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Gupta, M., Lee, H. J., Barden, C., & Weaver, D. F. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b01220 · Cited by 345

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Israel, L. L., Galstyan, A., Holler, E., & Ljubimova, J. Y. (2020) · Journal of Controlled Release · doi:10.1016/j.jconrel.2020.01.009 · Cited by 343

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Saeedi, M., Eslamifar, M., Khezri, K., & Dizaj, S. M. (2019) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2018.12.133 · Cited by 342

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Waring, M. J. (2009) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2009.03.109 · Cited by 340

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Yu, S., Xu, X., Feng, J., Liu, M., & Hu, K. (2019) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2019.02.012 · Cited by 340

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Wang, H., Sui, H., Zheng, Y., Jiang, Y., Shi, Y., Liang, J., & Zhao, L. (2019) · Nanoscale · doi:10.1039/c9nr01255a · Cited by 324

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Kealy, J., Greene, C., & Campbell, M. (2018) · Neuroscience Letters · doi:10.1016/j.neulet.2018.06.033 · Cited by 318

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Durant, S. T., Zheng, L., Wang, Y., Chen, K., Zhang, L., Zhang, T., Yang, Z., Riches, L. C., Trinidad, A. G., Fok, J. H. L., et al. (2018) · Science Advances · doi:10.1126/sciadv.aat1719 · Cited by 316

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Sun, H., Dai, H. I., Shaik, N. M., & Elmquist, W. F. (2003) · Advanced Drug Delivery Reviews · doi:10.1016/s0169-409x(02)00172-2 · Cited by 305

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He, Q., Liu, J., Liang, J., Liu, X., Li, W., Zhi, L., Ding, Z., & Tuo, D. (2018) · Cells · doi:10.3390/cells7040024 · Cited by 304

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Mikitsh, J. L., & Chacko, A. (2014) · Perspectives in Medicinal Chemistry · doi:10.4137/pmc.s13384 · Cited by 284

Comparison of brain capillary endothelial cell-based and epithelial (MDCK-MDR1, Caco-2, and VB-Caco-2) cell-based surrogate blood–brain barrier penetration models

Hellinger, É., Veszelka, S., Tóth, A. E., Walter, F. R., Kittel, Á., Bakk, M. L., Tihanyi, K., Háda, V., Nakagawa, S., Duy, T. D. H., et al. (2012) · European Journal of Pharmaceutics and Biopharmaceutics · doi:10.1016/j.ejpb.2012.07.020 · Cited by 251

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Huchet, Q. A., Kuhn, B., Wagner, B., Kratochwil, N. A., Fischer, H., Kansy, M., Zimmerli, D., Carreira, E. M., & Müller, K. (2015) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5b01455 · Cited by 241

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Agrawal, M., Saraf, S., Saraf, S., Dubey, S. K., Puri, A., Patel, R. J., Ajazuddin, M., Ravichandiran, V., Murty, U. S., & Alexander, A. (2020) · Journal of Controlled Release · doi:10.1016/j.jconrel.2020.02.020 · Cited by 239

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Hitchcock, S. A. (2012) · Journal of Medicinal Chemistry · doi:10.1021/jm201136z · Cited by 232

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Raub, T. J. (2005) · Molecular Pharmaceutics · doi:10.1021/mp0500871 · Cited by 221

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Charifson, P. S., & Walters, W. P. (2014) · Journal of Medicinal Chemistry · doi:10.1021/jm501000a · Cited by 216

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Röver, S., Cesura, A. M., Huguenin, P. N., Kettler, R., & Szente, A. (1997) · Journal of Medicinal Chemistry · doi:10.1021/jm970467t · Cited by 212

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Sivandzade, F., & Cucullo, L. (2018) · Journal of Cerebral Blood Flow & Metabolism · doi:10.1177/0271678x18788769 · Cited by 210

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Puris, E., Gynther, M., Auriola, S. O. K., & Huttunen, K. M. (2020) · Pharmaceutical Research · doi:10.1007/s11095-020-02826-8 · Cited by 206

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Sharma, G., Sharma, A. R., Lee, S., Bhattacharya, M., Nam, J., & Chakraborty, C. (2019) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2019.01.056 · Cited by 202

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Jena, L., McErlean, E. M., & McCarthy, H. O. (2019) · Drug Delivery and Translational Research · doi:10.1007/s13346-019-00679-2 · Cited by 182

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Walsh, D. M., & Selkoe, D. J. (2020) · Current Opinion in Neurobiology · doi:10.1016/j.conb.2020.02.003 · Cited by 164

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Singh, N., & Ecker, G. F. (2018) · International Journal of Molecular Sciences · doi:10.3390/ijms19051278 · Cited by 145

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Heffron, T. P. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b00618 · Cited by 144

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Kaisar, M. A., Sajja, R. K., Prasad, S., Abhyankar, V. V., Liles, T., & Cucullo, L. (2016) · Expert Opinion on Drug Discovery · doi:10.1080/17460441.2017.1253676 · Cited by 141

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Veszelka, S., Tóth, A., Walter, F. R., Tóth, A. E., Gróf, I., Mészáros, M., Bocsik, A., Hellinger, É., Vastag, M., Rákhely, G., et al. (2018) · Frontiers in Molecular Neuroscience · doi:10.3389/fnmol.2018.00166 · Cited by 141

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Bruno, O., Fedele, E., Prickaerts, J., Parker, L. A., Canepa, E., Brullo, C., Cavallero, A., Gardella, E., Balbi, A., Domenicotti, C., et al. (2011) · British Journal of Pharmacology · doi:10.1111/j.1476-5381.2011.01524.x · Cited by 137

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Shakeri, S., Ashrafizadeh, M., Zarrabi, A., Roghanian, R., Afshar, E. G., Pardakhty, A., Mohammadinejad, R., Kumar, A., & Thakur, V. K. (2020) · Biomedicines · doi:10.3390/biomedicines8010013 · Cited by 136

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Pettersson, M., Hou, X., Kühn, M., Wager, T. T., Kauffman, G. W., & Verhoest, P. R. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b00027 · Cited by 128

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Fernandes, J., & Gattass, C. R. (2009) · Journal of Medicinal Chemistry · doi:10.1021/jm801389m · Cited by 125

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Rai, G., Vyjayanti, V. N., Dorjsuren, D. G., Simeonov, A. M., Jadhav, A., Wilson, D. M., & Maloney, D. J. (2012) · Journal of Medicinal Chemistry · doi:10.1021/jm201537d · Cited by 123

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Di, L., Kerns, E. H., & Carter, G. T. (2008) · Expert Opinion on Drug Discovery · doi:10.1517/17460441.3.6.677 · Cited by 121

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Brand, S. L., Cleghorn, L. A. T., McElroy, S. P., Robinson, D. A., Smith, V. C., Hallyburton, I., Harrison, J. R., Norcross, N. R., Spinks, D., Bayliss, T., et al. (2011) · Journal of Medicinal Chemistry · doi:10.1021/jm201091t · Cited by 119

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Shidore, M. M., Machhi, J., Shingala, K., Murumkar, P. R., Sharma, M. K., Agrawal, N., Tripathi, A., Parikh, Z. S., Pillai, P. P., & Yadav, M. R. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b00426 · Cited by 114

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Reis, J., Cagide, F., Chavarria, D., Silva, T., Fernandes, C., Gaspar, A., Uriarte, E., Remião, F., Alcaro, S., Ortuso, F., et al. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b00527 · Cited by 111

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Feng, B., West, M. A., Patel, N. C., Wager, T. T., Hou, X., Johnson, J. G., Tremaine, L. M., & Liras, J. L. (2019) · Journal of Pharmaceutical Sciences · doi:10.1016/j.xphs.2019.02.005 · Cited by 107

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Li, Q., Xing, S., Chen, Y., Liao, Q., Xiong, B., He, S., Lu, W., Liu, Y., Yang, H., Li, Q., et al. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c01129 · Cited by 106

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Deo, A. K., Theil, F., & Nicolas, J.-M. (2012) · Molecular Pharmaceutics · doi:10.1021/mp300570z · Cited by 105

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Peauger, L., Azzouz, R., Gembus, V., Ţînţaş, M.-L., Santos, J. S. O., Bohn, P., Papamicaël, C. A., & Levacher, V. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.7b00702 · Cited by 99

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Vraka, C., Nics, L., Wagner, K., Hacker, M., Wadsak, W., & Mitterhauser, M. (2017) · Nuclear Medicine and Biology · doi:10.1016/j.nucmedbio.2017.03.003 · Cited by 94

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Puris, E., Gynther, M., Huttunen, J., Petsalo, A., & Huttunen, K. M. (2017) · Journal of Controlled Release · doi:10.1016/j.jconrel.2017.06.023 · Cited by 91

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Chien, H., Colas, C., Finke, K., Springer, S. D., Stoner, L., Zur, A. A., Venteicher, B., Campbell, J., Hall, C., Flint, A., et al. (2018) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b01007 · Cited by 88

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Li, X., Wang, H., Lu, Z., Zheng, X., Wei Min, N. I., Zhu, J., Fu, Y., Lian, F., Zhang, N., Li, J., et al. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b00636 · Cited by 83

L-Type Amino Acid Transporter 1 Enables the Efficient Brain Delivery of Small-Sized Prodrug across the Blood–Brain Barrier and into Human and Mouse Brain Parenchymal Cells

Montaser, A. B., Järvinen, J., Löffler, S., Huttunen, J., Auriola, S. O. K., Lehtonen, M., Jalkanen, A. J., & Huttunen, K. M. (2020) · ACS Chemical Neuroscience · doi:10.1021/acschemneuro.0c00564 · Cited by 70

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Jafari, B., Pourseif, M. M., Barar, J., Rafi, M. A., & Omidi, Y. (2019) · Expert Opinion on Drug Delivery · doi:10.1080/17425247.2019.1614911 · Cited by 65

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Hamdouchi, C., Kahl, S. D., Lewis, A. P., Cardona, G. R., Zink, R. W., Chen, K., Eessalu, T. E., FICORILLI, J. V., Marcelo, M. C., Otto, K. A., et al. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b00892 · Cited by 64

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Puris, E., Gynther, M., Huttunen, J., Auriola, S. O. K., & Huttunen, K. M. (2019) · European Journal of Pharmaceutical Sciences · doi:10.1016/j.ejps.2019.01.002 · Cited by 64

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Parvaz, S., Taheri‐Ledari, R., Esmaeili, M. S., Rabbani, M., & Maleki, A. R. (2019) · Life Sciences · doi:10.1016/j.lfs.2019.117099 · Cited by 64

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Zhao, Y., Qu, B., Wu, X., Li, X., Liu, Q., Jin, X., Guo, L., Hai, L., & Wu, Y. (2014) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2014.05.072 · Cited by 62

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Günaydin, H. (2015) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.5b00390 · Cited by 59

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Koriyama, Y., Hori, A., Ito, H., Yonezawa, S., Baba, Y., Tánimoto, N., Ueno, T., Yamamoto, S., Yamamoto, T., Asada, N., et al. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c01917 · Cited by 59

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Ohashi, R., Watanabe, R., Esaki, T., Taniguchi, T., Torimoto‐Katori, N., Watanabe, T., Ogasawara, Y., Takahashi, T., Tsukimoto, M., & Mizuguchi, K. (2019) · Molecular Pharmaceutics · doi:10.1021/acs.molpharmaceut.8b01143 · Cited by 57

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Wohlrab, C., Phillips, E., & Dachs, G. U. (2017) · Frontiers in Oncology · doi:10.3389/fonc.2017.00074 · Cited by 53

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Placzek, A. T., Ferrara, S. J., Hartley, M. D., Sanford-Crane, H. S., Meinig, J. M., & Scanlan, T. S. (2016) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2016.09.038 · Cited by 48

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Feng, B., Doran, A. C., Di, L., West, M. A., Osgood, S. M., Mancuso, J. Y., Shaffer, C. L., Tremaine, L. M., & Liras, J. L. (2018) · Journal of Pharmaceutical Sciences · doi:10.1016/j.xphs.2018.03.018 · Cited by 45

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Heffron, T. P. (2017) · Neuro-Oncology · doi:10.1093/neuonc/nox179 · Cited by 43

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Ghose, A. K., Ott, G. R., & Hudkins, R. L. (2016) · ACS Chemical Neuroscience · doi:10.1021/acschemneuro.6b00273 · Cited by 42

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Brullo, C., Ricciarelli, R., Prickaerts, J., Arancio, O., Massa, M., Rotolo, C., Romussi, A., Rebosio, C., Marengo, B., Pronzato, M. A., et al. (2016) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2016.08.018 · Cited by 41

Drug Distribution into Peripheral Nerve

Liu, H., Chen, Y., Huang, L. J., Sun, X., Fu, T., Wu, S., Zhu, X., Wei, Z. C., Liu, J., Lü, G., et al. (2018) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.117.245613 · Cited by 41

Rivastigmine and metabolite analogues with putative Alzheimer’s disease-modifying properties in a Caenorhabditis elegans model

Dighe, S. N., la Mora, E. D., Chan, S., Kantham, S., McColl, G., Miles, J. A., Veliyath, S. K., Sreenivas, B. Y., Nassar, Z. D., Silman, I., et al. (2019) · Communications Chemistry · doi:10.1038/s42004-019-0133-4 · Cited by 40

Development of a Potent Brain-Penetrant EGFR Tyrosine Kinase Inhibitor against Malignant Brain Tumors

Tsang, J., Urner, L. M., Kim, G., Chow, K. V., Baufeld, L., Faull, K. F., Cloughesy, T. F., Clark, P. M., Jung, M. E., & Nathanson, D. A. (2020) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.9b00599 · Cited by 40

Design, synthesis and biological evaluation of brain penetrant benzazepine-based histone deacetylase 6 inhibitors for alleviating stroke-induced brain infarction

Guo, Z., Zhang, Z., Zhang, Y., Wang, G., Huang, Z., Zhang, Q., & Li, J. (2021) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2021.113383 · Cited by 39

Hit-to-Lead Optimization of a Novel Class of Potent, Broad-Spectrum Trypanosomacides

Russell, S., Rahmani, R., Jones, A. J., Newson, H. L., Neildé, K., Cotillo, I., Khajouei, M. R., Ferrins, L., Qureishi, S., Nguyen, N. H., et al. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b00442 · Cited by 39

Systemic and Brain Pharmacokinetics of Perforin Inhibitor Prodrugs

Gynther, M., Pickering, D. S., Spicer, J. A., Denny, W. A., & Huttunen, K. M. (2016) · Molecular Pharmaceutics · doi:10.1021/acs.molpharmaceut.6b00217 · Cited by 38

Identification of human, rat and mouse hydrolyzing enzymes bioconverting amino acid ester prodrug of ketoprofen

Huttunen, K. M. (2018) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2018.09.018 · Cited by 36

Dihydroquinoline Carbamate Derivatives as “Bio-oxidizable” Prodrugs for Brain Delivery of Acetylcholinesterase Inhibitors: [11C] Radiosynthesis and Biological Evaluation

Bohn, P., Gourand, F., Papamicaël, C. A., Ibazizène, M., Dhilly, M., Gembus, V., Allix, F., Ţînţaş, M.-L., Marsais, F., Barré, L., et al. (2015) · ACS Chemical Neuroscience · doi:10.1021/cn5003539 · Cited by 35

GLUT 1 ‐mediated venlafaxine‐thiamine disulfide system‐glucose conjugates with “lock‐in” function for central nervous system delivery

Zhao, Y., Zhang, L., Yao, P., Yue, Q., Hai, L., Guo, L., Wang, Q., & Wu, Y. (2017) · Chemical Biology & Drug Design · doi:10.1111/cbdd.13128 · Cited by 33

Practical approaches to evaluating and optimizing brain exposure in early drug discovery

Freeman, B. B., Yang, L., & Ranković, Z. (2019) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2019.111643 · Cited by 31

Continued optimization of the M5 NAM ML375: Discovery of VU6008667, an M5 NAM with high CNS penetration and a desired short half-life in rat for addiction studies

McGowan, K. M., Nance, K. D., Cho, H. P., Bridges, T. M., Conn, P. J., Jones, C. K., & Lindsley, C. W. (2017) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2017.02.020 · Cited by 31

Real-Time Parallel Artificial Membrane Permeability Assay Based on Supramolecular Fluorescent Artificial Receptors

He, S., Zhiti, A., Barba‐Bon, A., Hennig, A., & Nau, W. M. (2020) · Frontiers in Chemistry · doi:10.3389/fchem.2020.597927 · Cited by 31

Mechanistic Study on the Use of the l -Type Amino Acid Transporter 1 for Brain Intracellular Delivery of Ketoprofen via Prodrug: A Novel Approach Supporting the Development of Prodrugs for Intracellular Targets

Puris, E., Gynther, M., de Lange, E. C. M., Auriola, S. O. K., Hammarlund‐Udenaes, M., Huttunen, K. M., & Loryan, I. (2019) · Molecular Pharmaceutics · doi:10.1021/acs.molpharmaceut.9b00502 · Cited by 30

Applicability of free drug hypothesis to drugs with good membrane permeability that are not efflux transporter substrates: A microdialysis study in rats

Chen, C., Zhou, H., Guan, C., Zhang, H., Li, Y., Jiang, X., Dong, Z., Tao, Y., Du, J., Wang, S., et al. (2020) · Pharmacology Research & Perspectives · doi:10.1002/prp2.575 · Cited by 30

Combined PET and microdialysis for in vivo estimation of drug blood-brain barrier transport and brain unbound concentrations

Gustafsson, S. S., Eriksson, J., Syvänen, S., Eriksson, O., Hammarlund‐Udenaes, M., & Antoni, G. (2017) · NeuroImage · doi:10.1016/j.neuroimage.2017.04.068 · Cited by 29

Novel derivatives of anaplastic lymphoma kinase inhibitors: Synthesis, radiolabeling, and preliminary biological studies of fluoroethyl analogues of crizotinib, alectinib, and ceritinib

Radaram, B., Pisaneschi, F., Rao, Y., Yang, P., Piwnica-Worms, D. R., & Alauddin, M. M. (2019) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2019.111571 · Cited by 29

Selective IKur Inhibitors for the Potential Treatment of Atrial Fibrillation: Optimization of the Phenyl Quinazoline Series Leading to Clinical Candidate 5-[5-Phenyl-4-(pyridin-2-ylmethylamino)quinazolin-2-yl]pyridine-3-sulfonamide

Gunaga, P., Lloyd, J., Mummadi, S., Banerjee, A., Dhondi, N. K., Hennan, J. K., Subray, V., Jayaram, R., Rajugowda, N., Reddy, K. U., et al. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b01889 · Cited by 25

Design and Synthesis of Brain Penetrant Trypanocidal N -Myristoyltransferase Inhibitors

Bayliss, T., Robinson, D. A., Smith, V. C., Brand, S. L., McElroy, S. P., Torrie, L. S., Mpamhanga, C., Norval, S., Stojanovski, L., Brenk, R., et al. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.7b01255 · Cited by 25

Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core

Wood, M. R., Noetzel, M. J., Engers, J. L., Bollinger, K. A., Melancon, B. J., Tarr, J. C., Han, C., West, M. K., Gregro, A. R., Lamsal, A., et al. (2016) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2016.05.010 · Cited by 23

Targeted Fluorination of a Nonsteroidal Anti‐inflammatory Drug to Prolong Metabolic Half‐Life

Shaughnessy, M. J., Harsányi, A., Li, J., Bright, T. V., Murphy, C. D., & Sandford, G. (2014) · ChemMedChem · doi:10.1002/cmdc.201300490 · Cited by 22

The Brain Exposure Efficiency (BEE) Score

Gupta, M., Bogdanowicz, T., Reed, M. A., Barden, C., & Weaver, D. F. (2019) · ACS Chemical Neuroscience · doi:10.1021/acschemneuro.9b00650 · Cited by 22

Exploiting Transport Activity of P-Glycoprotein at the Blood–Brain Barrier for the Development of Peripheral Cannabinoid Type 1 Receptor Antagonists

Wittgen, H. G. M., Greupink, R., van den Heuvel, J. J. M. W., van den Broek, P. H. H., Dinter-Heidorn, H., Koenderink, J. B., & Rüssel, F. G. M. (2012) · Molecular Pharmaceutics · doi:10.1021/mp200617z · Cited by 22

Discovery of Potent, Selective, and Brain-Penetrant 1H-Pyrazol-5-yl-1H-pyrrolo[2,3-b]pyridines as Anaplastic Lymphoma Kinase (ALK) Inhibitors

Fushimi, M., Fujimori, I., Wakabayashi, T., Hasui, T., Kawakita, Y., Imamura, K., Kato, T., Murakami, M., Ishii, T., Kikko, Y., et al. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b01630 · Cited by 22

Optimization of dipeptidic inhibitors of cathepsin L for improved Toxoplasma gondii selectivity and CNS permeability

Zwicker, J. D., Diaz, N. A., Guerra, A. J., Kirchhoff, P. D., Wen, B., Sun, D., Carruthers, V. B., & Larsen, S. D. (2018) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2018.03.020 · Cited by 21

VU6007477, a Novel M 1 PAM Based on a Pyrrolo[2,3- b ]pyridine Carboxamide Core Devoid of Cholinergic Adverse Events

Engers, J. L., Childress, E. S., Long, M. F., Capstick, R. A., Luscombe, V. B., Cho, H. P., Dickerson, J. W., Rook, J. M., Blobaum, A. L., Niswender, C. M., et al. (2018) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.8b00261 · Cited by 21

Novel application of capillary electrophoresis with a liposome coated capillary for prediction of blood-brain barrier permeability

Godyń, J., Gucwa, D., Kobrlová, T., Novak, M., Soukup, O., Malawska, B., & Bajda, M. (2020) · Talanta · doi:10.1016/j.talanta.2020.121023 · Cited by 21

Discovery, structure-activity relationship studies, and anti-nociceptive effects of N-(1,2,3,4-tetrahydro-1-isoquinolinylmethyl)benzamides as novel opioid receptor agonists

Chen, S.-R., Ke, Y., Yeh, T., Lin, S., Ou, L.-C., Chen, S.-C., Chang, W., Chang, H.-F., Wu, Z.-H., Hsieh, C.-C., et al. (2016) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2016.09.003 · Cited by 20

Selectivity and Physicochemical Optimization of Repurposed Pyrazolo[1,5- b ]pyridazines for the Treatment of Human African Trypanosomiasis

Tear, W. F., Bag, S., Díaz-González, R., Ceballos-Pérez, G., Rojas-Barros, D. I., Cordón-Obras, C., Pérez‐Moreno, G., García‐Hernández, R., Martínez, M. S., Ruiz-Pérez, L. M., et al. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b01741 · Cited by 19

Characterization of the neurotoxic potential of m-methoxy-MPTP and the use of its N-ethyl analog as a means of avoiding exposure to a possible Parkinson-causing agent

Zimmerman, D. M., Cantrell, B. E., Reel, J. K., Hemrick-Luecke, S. K., & Fuller, R. W. (1986) · Journal of Medicinal Chemistry · doi:10.1021/jm00158a033 · Cited by 18

Discovery and Optimization of Triazine Nitrile Inhibitors of Toxoplasma gondii Cathepsin L for the Potential Treatment of Chronic Toxoplasmosis in the CNS

Zwicker, J. D., Smith, D. W., Guerra, A. J., Hitchens, J. R., Haug, N., Roest, S. V., Lee, P. H., Wen, B., Sun, D., Wang, L., et al. (2020) · ACS Chemical Neuroscience · doi:10.1021/acschemneuro.9b00674 · Cited by 17

Discovery of 5-Phenyl-N-(pyridin-2-ylmethyl)-2-(pyrimidin-5-yl)quinazolin-4-amine as a PotentIKurInhibitor

Finlay, H. J., Johnson, J. A., Lloyd, J., Jiang, J., Neels, J. F., Gunaga, P., Banerjee, A., Dhondi, N. K., Chimalakonda, A., Mandlekar, S., et al. (2016) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.6b00117 · Cited by 16

N-(6-phenylpyridazin-3-yl)benzenesulfonamides as highly potent, brain-permeable, and orally active kynurenine monooxygenase inhibitors

Kimura, H., Suda, H., Kassai, M., Endo, M., Deai, Y., Yahata, M., Miyajima, M., & Isobe, Y. (2020) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2020.127753 · Cited by 15

The SAR of brain penetration for a series of heteroaryl urea FAAH inhibitors

Keith, J. M., Tichenor, M. S., Apodaca, R. L., Xiao, W., Jones, W. M., Seierstad, M. J., Pierce, J. M., Palmer, J. A., Webb, M., Karbarz, M. J., et al. (2016) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2016.05.001 · Cited by 12

Synthesis of a [18F]‐labeled ceritinib analogue for positron emission tomography of anaplastic lymphoma kinase, a receptor tyrosine kinase, in lung cancer

Perera, S., Piwnica-Worms, D. R., & Alauddin, M. M. (2016) · Journal of Labelled Compounds and Radiopharmaceuticals · doi:10.1002/jlcr.3373 · Cited by 12

Synthesis and in vitro , ex-vivo and in vivo activity of hybrid compounds linking a potent ROS and RNS scavenger activity with diverse substrates addressed to pass across the blood-brain barrier

Vázquez-Jiménez, L., Garrido, M., Miceli, M., Prats, E., Ferrer-Montiel, A. V., Teixidò, M., Jimeno, C., & Messeguer, Á. (2016) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2016.08.007 · Cited by 12

Discovery of a novel, CNS penetrant M4 PAM chemotype based on a 6-fluoro-4-(piperidin-1-yl)quinoline-3-carbonitrile core

Bewley, B. R., Spearing, P. K., Weiner, R. L., Luscombe, V. B., Zhan, X., Chang, S., Cho, H. P., Rodriguez, A. L., Niswender, C. M., Conn, P. J., et al. (2017) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2017.08.043 · Cited by 12

Developing RNA Aptamers for Potential Treatment of Neurological Diseases

Huang, Z., & Niu, L. (2019) · Future Medicinal Chemistry · doi:10.4155/fmc-2018-0364 · Cited by 11

Value of quantifying ABC transporters by mass spectrometry and impact on in vitro-to-in vivo prediction of transporter-mediated drug-drug interactions of rivaroxaban

Jacqueroux, E., Hodin, S., Saïb, S., Hé, Z., Bin, V., Delézay, O., & Delavenne, X. (2020) · European Journal of Pharmaceutics and Biopharmaceutics · doi:10.1016/j.ejpb.2020.01.002 · Cited by 11

Design, Synthesis and Evaluation of Dual-targeting Prodrug Co-modified by Organic Amine and L-ascorbic Acid for CNS Delivery

Qiu, S., Zhao, Y., Liu, S., Li, X., Guo, L., Hai, L., & Wu, Y. (2017) · Letters in Drug Design & Discovery · doi:10.2174/1570180814666161230161152 · Cited by 11

Design, synthesis and structure−activity relationship studies of GPR40 agonists containing amide linker

Chen, T., Ning, M., Ye, Y., Wang, K., Leng, Y., & Shen, J. (2018) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2018.04.023 · Cited by 11

Design, Synthesis and Enhanced BBB Penetration Studies of L-serine-Tethered Nipecotic Acid-Prodrug

Dhanawat, M., Gupta, S., Mehta, D., & Das, R. (2020) · Drug Research · doi:10.1055/a-1290-0119 · Cited by 11

Fibroblast growth factor receptor modulators employing diamines with reduced phospholipidosis-inducing potential

Sakai, H., Inoue, H., Murata, K., Toba, T., Shimmyo, Y., Narii, N., Ueno, S., Igawa, Y., & Takemoto, N. (2020) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2020.115562 · Cited by 11

A Practical Perspective on the Evaluation of Small Molecule CNS Penetration in Drug Discovery.

Huang, L.-Y., Wells, M. C., & Zhao, Z.-Y. (2020) · Drug Metabolism Letters · doi:10.2174/1872312813666190311125652 · Cited by 10

Altering Nitrogen Heterocycles of AZD2461 Affords High Affinity Poly(ADP-ribose) Polymerase-1 Inhibitors with Decreased P-Glycoprotein Interactions

Reilly, S. W., Puentes, L. N., Hsieh, C., Makvandi, M., & Mach, R. H. (2018) · ACS Omega · doi:10.1021/acsomega.8b00896 · Cited by 8

Microwave-assisted synthesis and in vitro stability of N-benzylamide non-steroidal anti-inflammatory drug conjugates for CNS delivery

Eden, B. D., Rice, A. J., Lovett, T. D., Toner, O. M., Geissler, E. P., Bowman, W. E., & Young, S. C. (2019) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2019.04.016 · Cited by 5

Blood–brain-barrier-crossing lipid nanoparticles for mRNA delivery to the central nervous system

Wang, C., Xue, Y., Markovic, T., Li, H., Wang, S., Zhong, Y., Du, S., Zhang, Y., Hou, X., Yu, Y., et al. (2025) · Nature Materials · doi:10.1038/s41563-024-02114-5 · Cited by 171

Explaining Blood–Brain Barrier Permeability of Small Molecules by Integrated Analysis of Different Transport Mechanisms

Cornelissen, F. M. G., Markert, G., Deutsch, G., Antonara, M., Faaij, N., Bartelink, I. H., Noske, D. P., Vandertop, W. P., Bender, A., & Westerman, B. A. (2023) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c01824 · Cited by 156

Extracellular Vesicles: A Review of Their Therapeutic Potentials, Sources, Biodistribution, and Administration Routes

Su, X., Wang, H., Li, Q., & Chen, Z. (2025) · International Journal of Nanomedicine · doi:10.2147/ijn.s502591 · Cited by 126

NLRP3 Inflammasome-Mediated Neuroinflammation and Related Mitochondrial Impairment in Parkinson’s Disease

Han, Q.-Q., & Le, W. (2023) · Neuroscience Bulletin · doi:10.1007/s12264-023-01023-y · Cited by 106

Differential Signaling Pathways in Medulloblastoma: Nano-biomedicine Targeting Non-coding Epigenetics to Improve Current and Future Therapeutics

Sokolov, D., Sharda, N., Banerjee, A., Denisenko, K., Basalious, E. B., Shukla, H. D., Waddell, J., Hamdy, N. Μ., & Banerjee, A. (2023) · Current Pharmaceutical Design · doi:10.2174/0113816128277350231219062154 · Cited by 72

Structure modification strategies to improve drug permeability of the blood-brain barrier

Li, Y. (2011) · Zhongguo yaowu huaxue zazhi

Breaking barriers: Medicinal chemistry strategies and advanced in-silico approaches for overcoming the BBB and enhancing CNS penetration

Ajayi, E. D., Elazazy, M., Abouzid, K. A. M., & Ali, H. I. (2025) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2025.118219 · Cited by 9

Medicinal chemistry strategies to breach the blood–brain barrier: structural design principles for brain-targeted therapeutics

Gupta, H. K., Jangra, J., Ramesh, V. K., Mahindru, I., & Kumar, R. (2026) · Drug Discovery Today · doi:10.1016/j.drudis.2026.104673 · Cited by 6

Blood-brain barrier permeability of small molecules: Mechanisms, determinants, and strategies for enhancing brain uptake

Gupta, A. G., Nagarale, S. N., Kadam, T., Gore, G., & Hole, G. (2026) · International Journal of Pharmaceutical and Clinical Research · doi:10.33545/26647591.2026.v8.i8a.218

Blood-Brain Barrier

Kerns, E. H., & Di, L. (2008) · Elsevier eBooks · doi:10.1016/b978-012369520-8.50011-5 · Cited by 14