Novel 2-aryl-naphtho[1,2-d]oxazole derivatives as potential PTP-1B inhibitors showing antihyperglycemic activities
Abstract
A series of 2-aryl-naphtho[1,2-d]oxazole derivatives have been synthesized and evaluated for PTP-1B inhibitory activity. The compounds have been screened in vivo for antidiabetic activity under sucrose loaded model (SLM), sucrose-challenged streptozotocin-induced diabetic rat model (STZ-S) and db/db mice model. Compounds 8 and 12 have shown promising PTP-1B inhibitory activity, significant antidiabetic activity, moderate lipid and triglyceride lowering activity.
Integrity signals
Registry
Cites
Statistics
Claims the paper makes
Claims other papers make about this one
Each is checked against this paper’s own text: does it say what the citing paper says it does?
Using adaptive emotion regulation strategies such as cognitive reappraisal can increase positive emotions and reduce negative emotions in stress, anxiety, depression, and mood swings.
“ّن چٌیي، اؾتفازُ اظ تطذی ضاّثطزّای ؾاظگاضاًِ تٌؾین ّیزاى ّوچَى اضظیاتی هزسز قٌاذتی زض هَارِْ تا اؾتطؼ، اضغطاب، افؿطزگی ٍ ًَؾاًات ذلمی زض تؿیاضی اظ هَالـ فلاٍُ تط واؾتي اظ ّیزاًات هٌفی، هیتَاًس ّیزاًات هخثت ضا افعایف زّس 43( ، )44 .”
From Effectiveness of Mindfulness Training in Emotion Regulation and Distress Tolerance among Breast Cancer Patients (2024) · cites this paper as [44]
Cites
Klaman, L. D., Boss, O., Peroni, O. D., Kim, J. K., Martino, J. L., Zabolotny, J. M., Moghal, N., Lubkin, M., Kim, Y.-B., Sharpe, A. H., et al. (2000) · Molecular and Cellular Biology · doi:10.1128/mcb.20.15.5479-5489.2000 · Cited by 1,235 · see citing works
Insulin Action, Diabetogenes, and the Cause of Type II Diabetes
Kahn, C. R. (1994) · Diabetes · doi:10.2337/diab.43.8.1066 · Cited by 916 · see citing works
Goldstein, B. J., Bittner-Kowalczyk, A., White, M. F., & Harbeck, M. C. (2000) · Journal of Biological Chemistry · doi:10.1074/jbc.275.6.4283 · Cited by 423 · see citing works
Malamas, M. S., Sredy, J., Moxham, C., Katz, A. H., Xu, W., McDevitt, R. E., Adebayo, F. O., Sawicki, D. R., Seestaller, L. M., Sullivan, D. S., et al. (2000) · Journal of Medicinal Chemistry · doi:10.1021/jm990560c · Cited by 216 · see citing works
Wrobel, J. E., Sredy, J., Moxham, C., Dietrich, A., Li, Z., Sawicki, D. R., Seestaller, L. M., Wu, L., Katz, A. H., Sullivan, D. S., et al. (1999) · Journal of Medicinal Chemistry · doi:10.1021/jm990260v · Cited by 125 · see citing works
Liljebris, C., Larsen, S. D., Ogg, D., Palazuk, B. J., & Bleasdale, J. E. (2002) · Journal of Medicinal Chemistry · doi:10.1021/jm011100y · Cited by 111 · see citing works
Recent development of small molecular specific inhibitor of protein tyrosine phosphatase 1B
Lee, S., & Wang, Q. (2006) · Medicinal Research Reviews · doi:10.1002/med.20079 · Cited by 109 · see citing works
Natural PTP1B Inhibitors from broussonetia papyrifera
Chen, R. M., Hu, L. H., An, T. Y., Li, J. X., & Shen, Q. (2002) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/s0960-894x(02)00757-6 · Cited by 102 · see citing works
Malamas, M. S., Sredy, J., Gunawan, I., Mihan, B., Sawicki, D. R., Seestaller, L. M., Sullivan, D. S., & Flam, B. R. (2000) · Journal of Medicinal Chemistry · doi:10.1021/jm990476x · Cited by 99 · see citing works
Prospects for Inhibitors of Protein Tyrosine Phosphatase 1B as Antidiabetic Drugs
van Huijsduijnen, R. H., Sauer, W., Bombrun, A., & Swinnen, D. (2004) · Journal of Medicinal Chemistry · doi:10.1021/jm030629n · Cited by 70 · see citing works
The development of potent non-peptidic PTP-1B inhibitors
Dufresne, C., Roy, P. J., Wang, Z., Asante‐Appiah, E., Cromlish, W. A., Boie, Y., Forghani, F., Desmarais, S., Wang, Q., Skorey, K., et al. (2004) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2003.11.048 · Cited by 70 · see citing works
Larsen, S. D., Barf, T. A., Liljebris, C., May, P. D., Ogg, D., O’Sullivan, T. J., Palazuk, B. J., Schostarez, H. J., Stevens, F. C., & Bleasdale, J. E. (2001) · Journal of Medicinal Chemistry · doi:10.1021/jm010393s · Cited by 66 · see citing works
Recent discovery and development of protein tyrosine phosphatase inhibitors
Kim, H.-O., & Blaskovich, M. A. T. (2002) · Expert Opinion on Therapeutic Patents · doi:10.1517/13543776.12.6.871 · Cited by 62 · see citing works
Cheon, H. G., Kim, S.-M., Yang, S., Ha, J. D., & Choi, J. (2004) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2003.11.070 · Cited by 38 · see citing works
PTP-1B inhibitors: Cyclopenta[d][1,2]-oxazine derivatives
Cho, S. Y., Baek, J. Y., Han, S. S., Kang, S. K., Ha, J. D., Ahn, J. H., Lee, J. D., Kim, K. R., Cheon, H. G., Rhee, S. D., et al. (2005) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2005.10.062 · Cited by 29 · see citing works
Flagged first, then by citations
Cited by
Sorted by citations
Protein Tyrosine Phosphatases as Drug Targets: Strategies and Challenges of Inhibitor Development
Barr, A. (2010) · Future Medicinal Chemistry · doi:10.4155/fmc.10.241 · Cited by 268 · see citing works
A comprehensive review on biological activities of oxazole derivatives
Kakkar, S., & Narasimhan, B. (2019) · BMC Chemistry · doi:10.1186/s13065-019-0531-9 · Cited by 225 · see citing works
Kumar, A., Srivastava, S., Gupta, G., Chaturvedi, V., Sinha, S. K., & Srivastava, A. K. (2010) · ACS Combinatorial Science · doi:10.1021/co100022h · Cited by 120 · see citing works
Self-citationSynthesis of chalcones and flavanones using Julia–Kocienski olefination
Kumar, A., Sharma, S., Tripathi, V. D., & Srivastava, S. (2010) · Tetrahedron · doi:10.1016/j.tet.2010.09.089 · Cited by 112 · see citing works
Self-citationKumar, A., Sharma, S., Tripathi, V. D., Maurya, R. A., Srivastava, S. P., Bhatia, G., Tamrakar, A. K., & Srivastava, A. K. (2009) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2009.11.061 · Cited by 104 · see citing works
Self-citationOxazole and isoxazole: From one-pot synthesis to medical applications
Thakur, A., Verma, M., Bharti, R., & Sharma, R. (2022) · Tetrahedron · doi:10.1016/j.tet.2022.132813 · Cited by 76 · see citing works
D‐Psicose, a Sweet Monosaccharide, Ameliorate Hyperglycemia, and Dyslipidemia in C57BL/6J db/db Mice
Baek, S. H., Park, S. J., & LEE, H. G. (2010) · Journal of Food Science · doi:10.1111/j.1750-3841.2009.01434.x · Cited by 68 · see citing works
Singh, S., Grewal, A. S., Grover, R., Sharma, N., Chopra, B., Dhingra, A. K., Arora, S., Redhu, S., & Lather, V. (2022) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2022.105626 · Cited by 67 · see citing works
PTP1B inhibitor improves both insulin resistance and lipid abnormalities in vivo and in vitro
Ma, Y.-M., Tao, R.-Y., Liu, Q., Li, J., Tian, J.-Y., Zhang, X.-L., Xiao, Z.-Y., & Ye, F. (2011) · Molecular and Cellular Biochemistry · doi:10.1007/s11010-011-0876-4 · Cited by 62 · see citing works
Kumar, A., Maurya, R. A., Sharma, S., Ahmad, P., Singh, A. B., Tamrakar, A. K., & Srivastava, A. K. (2009) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2009.05.033 · Cited by 54 · see citing works
Self-citationCalix[4]arene methylenebisphosphonic acids as inhibitors of protein tyrosine phosphatase 1B
Trush, V. V., Cherenok, S. О., Tanchuk, V. Y., Kukhar, V. P., Kаlchеnkо, V. I., & Vovk, A. I. (2013) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2013.08.040 · Cited by 43 · see citing works
Deb, M. L., Pegu, C. D., Borpatra, P. J., & Baruah, P. K. (2016) · RSC Advances · doi:10.1039/c6ra04567g · Cited by 40 · see citing works
Gold-catalyzed oxazoles synthesis and their relevant antiproliferative activities
Wu, C., Liang, Z., Xu, Y., He, W., & Xiang, J. (2013) · Chinese Chemical Letters · doi:10.1016/j.cclet.2013.06.026 · Cited by 36 · see citing works
Kumar, A., Gupta, M., & Kumar, M. (2012) · RSC Advances · doi:10.1039/c2ra20848b · Cited by 36 · see citing works
Self-citationDesign, synthesis and biological evaluation of 3-(2-aminooxazol-5-yl)-2H-chromen-2-one derivatives
Kakkar, S., Kumar, S., Lim, S. M., Ramasamy, K., Mani, V., Shah, S. A. A., & Narasimhan, B. (2018) · Chemistry Central Journal · doi:10.1186/s13065-018-0499-x · Cited by 33 · see citing works
Šagud, I., Faraguna, F., Marinić, Ž., & Šindler‐Kulyk, M. (2011) · The Journal of Organic Chemistry · doi:10.1021/jo1025942 · Cited by 31 · see citing works
Fullerene derivatives as a new class of inhibitors of protein tyrosine phosphatases
Kobzar, O. L., Trush, V. V., Tanchuk, V. Y., Zhilenkov, A. V., Troshin, P. A., & Vovk, A. I. (2014) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2014.04.110 · Cited by 30 · see citing works
Aljaar, N., Malakar, C. C., Conrad, J., Frey, W. U., & Beifuß, U. (2012) · The Journal of Organic Chemistry · doi:10.1021/jo3022956 · Cited by 30 · see citing works
Gao, S., Gao, L., Meng, H., Luo, M., & Zeng, X. (2017) · Chemical Communications · doi:10.1039/c7cc04965j · Cited by 29 · see citing works
Suh, J. H., Yum, E. K., & Cho, Y. S. (2015) · Chemical and Pharmaceutical Bulletin · doi:10.1248/cpb.c15-00033 · Cited by 23 · see citing works
Review on Chemistry of Oxazole derivatives: Current to Future Therapeutic Prospective
Joshi, S., Mehra, M., Singh, R., & Kakar, S. (2023) · Egyptian Journal of Basic and Applied Sciences · doi:10.1080/2314808x.2023.2171578 · Cited by 21 · see citing works
Synthesis of Naphthoxazoles by Photocyclization of 4‐/5‐(Phenylethenyl)oxazoles
Šagud, I., Šindler‐Kulyk, M., Škorić, I., Kelava, V., & Marinić, Ž. (2018) · European Journal of Organic Chemistry · doi:10.1002/ejoc.201800737 · Cited by 20 · see citing works
Kumari, R., Varghese, A., & George, L. (2016) · Journal of Fluorescence · doi:10.1007/s10895-016-1942-9 · Cited by 19 · see citing works
Phatangare, K. R., Borse, B. N., Padalkar, V. S., Patil, V. S., Gupta, V. D., Umape, P. G., & Sekar, N. (2013) · Journal of Chemical Sciences · doi:10.1007/s12039-012-0324-3 · Cited by 20 · see citing works
Kumari, R., Varghese, A., & George, L. (2016) · Journal of Luminescence · doi:10.1016/j.jlumin.2016.07.022 · Cited by 18 · see citing works
Arshad, M. (2018) · Russian Journal of General Chemistry · doi:10.1134/s1070363218090207 · Cited by 17 · see citing works
Classification of Binding Site Conformations of Protein Tyrosine Phosphatase 1B
Tanchuk, V. Y., Tanin, V. O., & Vovk, A. I. (2012) · Chemical Biology & Drug Design · doi:10.1111/j.1747-0285.2012.01370.x · Cited by 16 · see citing works
Atahan, A., & Durmuş, S. (2015) · Spectrochimica Acta Part A Molecular and Biomolecular Spectroscopy · doi:10.1016/j.saa.2015.01.085 · Cited by 16 · see citing works
Prasad, K. V., Saidachary, G., Kurma, S. H., Nagaraju, P., Rao, V. J., & Raju, B. C. (2016) · Asian Journal of Organic Chemistry · doi:10.1002/ajoc.201600131 · Cited by 15 · see citing works
Arshad, M. (2020) · SN Applied Sciences · doi:10.1007/s42452-020-2243-0 · Cited by 14 · see citing works
Szabó, T., Dancsó, A., Ábrányi‐Balogh, P., Volk, B., & Milen, M. (2019) · Tetrahedron Letters · doi:10.1016/j.tetlet.2019.04.024 · Cited by 12 · see citing works
Hydrogen bonded complexes of oxazole family: electronic structure, stability, and reactivity aspects
Chopra, N., Kaur, D., & Chopra, G. (2017) · Structural Chemistry · doi:10.1007/s11224-017-1032-x · Cited by 12 · see citing works
Kumar, A., Sharma, S., Gupta, L. P., Ahmad, P., Srivastava, S. P., Rahuja, N., Tamrakar, A. K., & Srivastava, A. K. (2011) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2011.12.027 · Cited by 10 · see citing works
Self-citationMicrowave-Assisted Synthesis of Heterocyclic Scaffolds
Agarwal, A., Kumar, S., & Maurya, A. (2024) · SynOpen · doi:10.1055/s-0043-1775379 · Cited by 9 · see citing works
Noruzpour, M., Zakaria, R. A., Zare, N., Ebrahimi, H. A., Khankandi, H. P., & Bourang, S. (2024) · Journal of Breast Disease · doi:10.61186/ijbd.17.1.59 · Cited by 6 · see citing works
Obernikhina, N., Kobzar, O. L., Kachaeva, M. V., Kachkovsky, O. D., & Броварец, В. С. (2022) · Current Computer - Aided Drug Design · doi:10.2174/1573409918666220404100022 · Cited by 6 · see citing works
Malla, P., Kumar, R., Mattewal, S. K., Mahapatra, M. K., & Kumar, M. (2013) · Medicinal Chemistry Research · doi:10.1007/s00044-013-0690-5 · Cited by 6 · see citing works
Parsons, N. S., Lam, M. H., & Hamilton, S. E. (2012) · Journal of Forensic Sciences · doi:10.1111/j.1556-4029.2012.02283.x · Cited by 5 · see citing works
A series of 2, 4, 5-trisubstituted oxazole: Synthesis, characterization and DFT modelling
Kadam, V. S., Shaikh, S. G., & Patel, A. L. (2016) · Journal of Molecular Structure · doi:10.1016/j.molstruc.2016.02.033 · Cited by 5 · see citing works
DESIGN, SYNTHESIS AND ANTIBACTERIAL EVALUATION OF SOME NEW COUMARIN FUSED OXAZOLE DERIVATIVES
Kumar, P., Kapoor, R. P., Kumar, A., Rai, S. M., & Nayak, P. (2022) · INDIAN DRUGS · doi:10.53879/id.59.12.12710 · Cited by 3 · see citing works
Self-citationGornostaev, L. M., Khalyavina, Y. G., Lavrikova, T. I., Gatilov, Y. V., Stashina, G. A., & Firgang, S. I. (2014) · Russian Journal of Organic Chemistry · doi:10.1134/s1070428014120173 · Cited by 3 · see citing works
Kumar, S., Kajol, K., Nayak, P., Kumar, A., & Ramesh, C. (2022) · Chemistry - An Asian Journal · doi:10.1002/asia.202201151 · Cited by 2 · see citing works
Self-citationMalla, P., Kumar, R., & Kumar, M. (2012) · Journal of Chemometrics · doi:10.1002/cem.2480 · Cited by 2 · see citing works
D’souza, A., Kumar, P., Kumar, A., Rai, S. M., & Nayak, P. (2021) · Journal of Pharmaceutical Research International · doi:10.9734/jpri/2021/v33i35a31882 · Cited by 2 · see citing works
Self-citationBerber, H., & Uysal, Ü. D. (2015) · Anadolu Üniversitesi Bilim Ve Teknoloji Dergisi - B Teorik Bilimler · doi:10.20290/btdb.31629 · Cited by 2 · see citing works
1,3-Oxazol-4-ylphosphonium salts as new non-peptide inhibitors of furin
Osadchuk, T. V., Vk, K., & Shybyryn, O. V. (2019) · The Ukrainian Biochemical Journal · doi:10.15407/ubj91.04.005 · Cited by 1 · see citing works
Šagud, I., Ratković, A., Cedilak, M., Bosnar, M., Kelava, V., & Škorić, I. (2019) · Croatica Chemica Acta · doi:10.5562/cca3530 · Cited by 1 · see citing works
Parsaee, S., Jahani, N., Salehiniya, H., & Raeison, M. (2024) · Journal of Breast Diseases · doi:10.61186/ijbd.17.1.84
Kumar, A., Ahmad, P., Maurya, R. A., Singh, A. B., & Srivastava, A. K. (2009) · ChemInform · doi:10.1002/chin.200919125
Self-citationBiochemical and molecular targets of novel antidiabetic agents
Singh, A. B. (2009) · INFLIBNET
Self-citationEmerging Therapeutic Targets for Diabetes
(2016) · CRC Press eBooks · doi:10.1201/9781315370118-4
Toledano‐Magaña, Y., Néquiz, M., Valenzuela-Salas, L. M., Sánchez-García, J. J., Galindo‐Murillo, R., García‐Ramos, J. C., & Klimova, E. I. (2023) · Molecules · doi:10.3390/molecules28166008
Sukanya, S. H., Venkatesh, T., Upendranath, K., Shanavaz, H., & Nagaraj, O. (2024) · Pharmaceutical Chemistry Journal · doi:10.1007/s11094-024-03162-6
Oxazole Analogues as Potential Therapeutic Agents: A Comprehensive Review
Goel, N., Mudgil, S., Kasnia, R., Demiwal, S., & Nehra, B. (2025) · Pharmaceutical Fronts · doi:10.1055/a-2728-8329
- Authors
- Kumar, A., Ahmad, P., Maurya, R. A., Singh, A. B., & Srivastava, A. K.
- Affiliations
- Central Drug Research Institute (IN)
- Corresponding author
- Kumar, Atul
- Venue
- European Journal of Medicinal Chemistry
- Publisher
- Elsevier BV
- Published
- 2009-01
- Volume
- 44
- Issue
- 1
- Pages
- 109-116
- ISSN
- 0223-5234 (ISSN-L)
- OpenAlex
- W2952023935
- Cited by
- 54
- References
- 15
- Citations by year
- 2025: 1 · 2024: 4 · 2023: 2 · 2022: 5 · 2021: 1 · 2020: 1 · 2019: 4 · 2018: 3 · 2017: 2 · 2016: 6 · 2015: 3 · 2014: 2 · 2013: 4 · 2012: 5
- FWCI
- 1.78
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- European Journal of Medicinal Chemistry (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Tyrosine Phosphatases
- Physical Sciences › Chemistry › Organic Chemistry › Synthesis and biological activity
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Natural Antidiabetic Agents Studies
- Keywords
- PTP1B, antidiabetic activity, streptozotocin-induced diabetes, db/db mice, hypolipidemic activity, triglyceride lowering
- MeSH terms
- Animals, Diabetes Mellitus, Experimental, Enzyme Inhibitors, Hypoglycemic Agents, Lipids, Oxazoles, Structure-Activity Relationship, Triglycerides, Mice, Rats, Protein Tyrosine Phosphatase, Non-Receptor Type 1
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
Are you an author, or do you see a problem with this page? Request a review