From 2000 to Mid-2010: A Fruitful Decade for the Synthesis of Pyrazoles

Recent Developments in Isocyanide Based Multicomponent Reactions in Applied Chemistry

Dömling, A. (2006) · Chemical Reviews · doi:10.1021/cr0505728 · Cited by 4,106

1,3-Dipolar Cycloaddition Chemistry

Padwa, A. (1984) · Medical Entomology and Zoology · Cited by 3,241

Modern Synthetic Methods for Copper‐Mediated C(aryl)O, C(aryl)N, and C(aryl)S Bond Formation

Ley, S. V., & Thomas, A. W. (2003) · Angewandte Chemie International Edition · doi:10.1002/anie.200300594 · Cited by 2,554

Copper-Mediated Coupling Reactions and Their Applications in Natural Products and Designed Biomolecules Synthesis

Evano, G., Blanchard, N., & Toumi, M. (2008) · Chemical Reviews · doi:10.1021/cr8002505 · Cited by 2,138

Synthesis and Biological Evaluation of the 1,5-Diarylpyrazole Class of Cyclooxygenase-2 Inhibitors: Identification of 4-[5-(4-Methylphenyl)-3- (trifluoromethyl)-1 H-pyrazol-1-yl]benzenesulfonamide (SC-58635, Celecoxib)

Penning, T. D., Talley, J. J., Bertenshaw, S. R., Carter, J. S., Collins, P. W., Docter, S., Graneto, M. J., Lee, L. F., Malecha, J. W., Miyashiro, J. M., et al. (1997) · Journal of Medicinal Chemistry · doi:10.1021/jm960803q · Cited by 1,965

A General and Efficient Copper Catalyst for the Amidation of Aryl Halides and the N-Arylation of Nitrogen Heterocycles

Klapars, A., Antilla, J. C., Huang, X., & Buchwald, S. L. (2001) · Journal of the American Chemical Society · doi:10.1021/ja016226z · Cited by 1,021

Boronic Acids: Preparation and Applications in Organic Synthesis and Medicine

(2005) · Wiley eBooks · doi:10.1002/3527606548 · Cited by 984

Pyrazole Ligands: Structure−Affinity/Activity Relationships and Estrogen Receptor-α-Selective Agonists

Stauffer, S. R., Coletta, C. J., Tedesco, R., Nishiguchi, G., Carlson, K., Sun, J., Katzenellenbogen, B. S., & Katzenellenbogen, J. A. (2000) · Journal of Medicinal Chemistry · doi:10.1021/jm000170m · Cited by 760

Amino Acid Promoted CuI-Catalyzed C−N Bond Formation between Aryl Halides and Amines or N-Containing Heterocycles

Zhang, H., Cai, Q., & Ma, D. (2005) · The Journal of Organic Chemistry · doi:10.1021/jo0504464 · Cited by 644

Highly Efficient and Mild Copper‐Catalyzed N‐ and C‐Arylations with Aryl Bromides and Iodides

Cristau, H., Cellier, P. P., Spindler, J., & Taillefer, M. (2004) · Chemistry – A European Journal · doi:10.1002/chem.200400582 · Cited by 586

Structure−Activity Relationships of Pyrazole Derivatives as Cannabinoid Receptor Antagonists

Lan, R., Liu, Q., Fan, P., Lin, S., Fernando, S. R., McCallion, D., Pertwee, R., & Makriyannis, A. (1999) · Journal of Medicinal Chemistry · doi:10.1021/jm980363y · Cited by 447

Design, synthesis and biological evaluation of some pyrazole derivatives as anti-inflammatory-antimicrobial agents

Bekhit, A. A., & Abdel-Aziem, T. (2004) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2004.01.037 · Cited by 433

Novel 1,5-Diphenylpyrazole Nonnucleoside HIV-1 Reverse Transcriptase Inhibitors with Enhanced Activity versus the Delavirdine-Resistant P236L Mutant: Lead Identification and SAR of 3- and 4-Substituted Derivatives

Genin, M. J., Biles, C., Keiser, B. J., Poppe, S. M., Swaney, S. M., Tarpley, W. G., Yagi, Y., & Romero, D. L. (2000) · Journal of Medicinal Chemistry · doi:10.1021/jm990383f · Cited by 375

Domino Cu‐Catalyzed CN Coupling/Hydroamidation: A Highly Efficient Synthesis of Nitrogen Heterocycles

Martín, R., Rodríguez Rivero, M., & Buchwald, S. L. (2006) · Angewandte Chemie International Edition · doi:10.1002/anie.200602917 · Cited by 368

Identification of N-(4-Piperidinyl)-4-(2,6-dichlorobenzoylamino)-1 H-pyrazole-3-carboxamide (AT7519), a Novel Cyclin Dependent Kinase Inhibitor Using Fragment-Based X-Ray Crystallography and Structure Based Drug Design

Wyatt, P. G., Woodhead, A. J., Berdini, V., Boulstridge, J. A., Carr, M. G., Cross, D. M., Davis, D. J., Devine, L. A., Early, T. R., Feltell, R. E., et al. (2008) · Journal of Medicinal Chemistry · doi:10.1021/jm800382h · Cited by 340

Synthesis and biological evaluation of chalcones and their derived pyrazoles as potential cytotoxic agents

Bhat, B. A., Dhar, K. L., Puri, S. C., Saxena, A. K., Shanmugavel, M., & Qazi, G. N. (2005) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2005.03.121 · Cited by 274

Iron‐Catalyzed N‐Arylation of Nitrogen Nucleophiles

Correa, A., & Bolm, C. (2007) · Angewandte Chemie International Edition · doi:10.1002/anie.200703299 · Cited by 260

Novel, Potent Small-Molecule Inhibitors of the Molecular Chaperone Hsp90 Discovered through Structure-Based Design

Dymock, B. W., Barril, X., Brough, P. A., Cansfield, J. E., Massey, A., McDonald, E., Hubbard, R. E., Surgenor, A., Roughley, S. D., Webb, P., et al. (2005) · Journal of Medicinal Chemistry · doi:10.1021/jm050355z · Cited by 227

Design and Synthesis of Celecoxib and Rofecoxib Analogues as Selective Cyclooxygenase-2 (COX-2) Inhibitors: Replacement of Sulfonamide and Methylsulfonyl Pharmacophores by an Azido Bioisostere

Habeeb, A. G., Praveen Rao, P. N., & Knaus, E. E. (2001) · Journal of Medicinal Chemistry · doi:10.1021/jm010153c · Cited by 215

Convenient access to 1,3,4-trisubstituted pyrazoles carrying 5-nitrothiophene moiety via 1,3-dipolar cycloaddition of sydnones with acetylenic ketones and their antimicrobial evaluation

Rai, N. S., Kalluraya, B., Lingappa, B., Shenoy, S., & Puranic, V. G. (2007) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2007.08.002 · Cited by 156

Substituent Effects ofN-(1,3-Diphenyl-1H-pyrazol-5-yl)benzamides on Positive Allosteric Modulation of the Metabotropic Glutamate-5 Receptor in Rat Cortical Astrocytes

de Paulis, T., Hemstapat, R., Chen, Y., Zhang, Y., Saleh, S., Alagille, D., Baldwin, R. M., Tamagnan, G. D., & Conn, P. J. (2006) · Journal of Medicinal Chemistry · doi:10.1021/jm051252j · Cited by 133

Synthesis of New Fluorinated Tebufenpyrad Analogs with Acaricidal Activity Through Regioselective Pyrazole Formation

Fustero, S., Román, R., Sanz‐Cervera, J. F., Simón‐Fuentes, A., Bueno, J., & Villanova, S. (2008) · The Journal of Organic Chemistry · doi:10.1021/jo801729p · Cited by 130

Synthesis, Structure−Activity Relationship, and Evaluation of SR141716 Analogues: Development of Central Cannabinoid Receptor Ligands with Lower Lipophilicity

Katoch‐Rouse, R., Pavlova, O. A., Caulder, T., et al. (2003) · Journal of Medicinal Chemistry · doi:10.1021/jm020157x · Cited by 129

Three‐Component Reaction Using the Bestmann–Ohira Reagent: A Regioselective Synthesis of Phosphonyl Pyrazole Rings

Mohanan, K., Martin, A. R., TOUPET, L. J., Smietana, M., & Vasseur, J. (2010) · Angewandte Chemie International Edition · doi:10.1002/anie.200906781 · Cited by 122

Synthesis of pyrazoles through catalyst-free cycloaddition of diazo compounds to alkynes

Vuluga, D., Legros, J., Crousse, B., & Bonnet‐Delpon, D. (2008) · Green Chemistry · doi:10.1039/b812242c · Cited by 117

Copper‐Promoted Cycloaddition of Diazocarbonyl Compounds and Acetylides

Qi, X., & Ready, J. M. (2007) · Angewandte Chemie International Edition · doi:10.1002/anie.200700069 · Cited by 107

Pyrazole NNRTIs 4: Selection of UK-453,061 (lersivirine) as a Development Candidate

Mowbray, C. E., Burt, C., Corbau, R., Gayton, S., Hawes, M., Perros, M., Tran, I., Price, D. A., Quinton, F., Selby, M. D., et al. (2009) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2009.08.080 · Cited by 104

New Flexible Synthesis of Pyrazoles with Different, Functionalized Substituents at C3 and C5

Grotjahn, D. B., Van, S., Combs, D., Lev, D. A., Schneider, C., Rideout, M. C., Meyer, C., Hernandez, G., & Mejorado, L. H. (2002) · The Journal of Organic Chemistry · doi:10.1021/jo026083e · Cited by 103

An Ullmann Coupling of Aryl Iodides and Amines Using an Air-Stable Diazaphospholane Ligand

Yang, M., & Liu, F. (2007) · The Journal of Organic Chemistry · doi:10.1021/jo0712291 · Cited by 89

Chemo- and regioselectivity in the reactions between highly electrophilic fluorine containing dicarbonyl compounds and amines. Improved synthesis of the corresponding imines/enamines

Ohkura, H., Berbasov, D. O., & Soloshonok, V. A. (2003) · Tetrahedron · doi:10.1016/s0040-4020(03)00138-8 · Cited by 89

Synthesis and binding affinity of new pyrazole and isoxazole derivatives as potential atypical antipsychotics

Barceló, M., Raviña, E., Masaguer, C. F., Domínguez, E., Areias, F. M., Brea, J. M., & Loza, M. I. (2007) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2007.06.045 · Cited by 78

Synthesis and Selective Cyclooxygenase-2 Inhibitory Activity of a Series of Novel, Nitric Oxide Donor-Containing Pyrazoles

Ranatunge, R. R., Augustyniak, M. E., Bandarage, U. K., Earl, R. A., Ellis, J. L., Garvey, D. S., Janero, D. R., Letts, L. G., Martino, A. M., Murty, M. G., et al. (2004) · Journal of Medicinal Chemistry · doi:10.1021/jm030276s · Cited by 78

Facile synthesis of 2H-indazole derivatives starting from the Baylis–Hillman adducts of 2-cyclohexen-1-one

Lee, K. Y., Gowrisankar, S., & Kim, J. N. (2005) · Tetrahedron Letters · doi:10.1016/j.tetlet.2005.05.149 · Cited by 78

Discovery of 1-(2-Aminomethylphenyl)-3-trifluoromethyl-N- [3-fluoro-2‘-(aminosulfonyl)[1,1‘-biphenyl)]-4-yl]-1H-pyrazole-5-carboxyamide (DPC602), a Potent, Selective, and Orally Bioavailable Factor Xa Inhibitor

Pruitt, J. R., Pinto, D. J. P., Galemmo, R. A., Alexander, R., Rossi, K. A., Wells, B. L., Drummond, S., Bostrom, L. L., Burdick, D., Brückner, R., et al. (2003) · Journal of Medicinal Chemistry · doi:10.1021/jm030212h · Cited by 76

1,3-Diarylcycloalkanopyrazoles and diphenyl hydrazides as selective inhibitors of cyclooxygenase-2

Sui, Z., Guan, J., Ferro, M. P., McCoy, K., Wachter, M. P., Murray, W. V., Singer, M. M., Steber, M., Ritchie, D. M., & Argentieri, D. C. (2000) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/s0960-894x(00)00041-x · Cited by 76

New Bis(chalcones) and Their Transformation into Bis(pyrazoline) and Bis(pyrazole) Derivatives

Pinto, D. C. G. A., Silva, A. M. S., Cavaleiro, J. A. S., & Elguero, J. (2003) · European Journal of Organic Chemistry · doi:10.1002/ejoc.200390117 · Cited by 66

Regioselective synthesis of fluorinated pyrazole derivatives from trifluoromethyl-1,3-diketone

Song, L.-P., & Zhu, S. (2001) · Journal of Fluorine Chemistry · doi:10.1016/s0022-1139(01)00454-7 · Cited by 62

Ligand‐Based Virtual Screening, Parallel Solution‐Phase and Microwave‐Assisted Synthesis as Tools to Identify and Synthesize New Inhibitors of Mycobacterium tuberculosis

Manetti, F., Magnani, M., Castagnolo, D., Passalacqua, L., Botta, M., Corelli, F., Saddi, M., Deidda, D., & Logu, A. D. (2006) · ChemMedChem · doi:10.1002/cmdc.200600026 · Cited by 47

Synthesis and anti-microbial activity of some new fluorinated 1H-pyrazoles

Wang, D., Fan, L., Zheng, C.-Y., & Fang, Z. (2010) · Journal of Fluorine Chemistry · doi:10.1016/j.jfluchem.2010.01.005 · Cited by 36

Design, synthesis and biological evaluation of new potent and highly selective ROS1-tyrosine kinase inhibitor

Park, B. S., El-Deeb, I. M., Yoo, K. H., Oh, C., Cho, S. J., Han, D. K., Lee, H., Lee, J. Y., & Lee, S. H. (2009) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2009.06.066 · Cited by 36

Synthesis and biological evaluation of 2-pyridyl-substituted pyrazoles and imidazoles as transforming growth factor-β type 1 receptor kinase inhibitors

Dewang, P. M., & Kim, D. (2010) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2010.05.032 · Cited by 34

A facile and convenient approach to the synthesis of 3,5-diaryl-1H-pyrazoles

Nikpour, F., & Beigvand, M. (2008) · Monatshefte für Chemie - Chemical Monthly · doi:10.1007/s00706-007-0829-5 · Cited by 11

1,3,4-Thiadiazole: Synthesis, Reactions, and Applications in Medicinal, Agricultural, and Materials Chemistry

Hu, Y., Li, C.-Y., Wang, X.-M., Yang, Y.-H., & Zhu, H.-L. (2014) · Chemical Reviews · doi:10.1021/cr400131u · Cited by 607

Coordination polymers and metal–organic frameworks based on poly(pyrazole)-containing ligands

Pettinari, C., Tăbăcaru, A., & Galli, S. (2016) · Coordination Chemistry Reviews · doi:10.1016/j.ccr.2015.08.005 · Cited by 269

Decoupling Activation of Heme Biosynthesis from Anaerobic Toxicity in a Molecule Active in Staphylococcus aureus

Dutter, B. F., Mike, L. A., Reid, P. R., Chong, K. M., Ramos-Hunter, S. J., Skaar, E. P., & Sulikowski, G. A. (2016) · ACS Chemical Biology · doi:10.1021/acschembio.5b00934 · Cited by 14