Synthesis and biological evaluation of N-substituted-3,5-diphenyl-2-pyrazoline derivatives as cyclooxygenase (COX-2) inhibitors

被引：117
作者：
Fioravanti, Rossella [1 ]
Bolasco, Adriana [1 ]
Manna, Fedele [1 ]
Rossi, Francesca [1 ]
Orallo, Francisco [2 ,3 ]
Ortuso, Francesco [4 ]
Alcaro, Stefano [4 ]
Cirilli, Roberto [5 ]
机构：
[1] Univ Roma La Sapienza, Dipartimento Chim & Tecnol Farm, I-00185 Rome, Italy
[2] Univ Santiago de Compostela, Fac Farm, Dept Farmacol, E-15782 Santiago De Compostela, La Coruna, Spain
[3] Univ Santiago de Compostela, Fac Farm, Inst Farm Ind, E-15782 Santiago De Compostela, La Coruna, Spain
[4] Univ Catanzaro Magna Graecia, Dipartimento Sci Farmacobiol, I-88021 Roccelletta Di Borgia, CZ, Italy
[5] Ist Super Sanita, Dipartimento Farm, I-00161 Rome, Italy
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 45卷 / 12期
关键词：
Pyrazoline; COX inhibitors; Molecular modeling; NONSTEROIDAL ANTIINFLAMMATORY DRUGS; STEREOSELECTIVE RECOGNITION MECHANISMS; MONOAMINE-OXIDASE; SYNTHASE-1; DOCKING; SELECTIVITY; FUTURE; AGENTS;
D O I：
10.1016/j.ejmech.2010.10.005
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Eighteen new 1-N-substituted-3,5-diphenyl-2-pyrazoline derivatives have been synthesized and cyclooxygenase (COX-1 and COX-2) inhibitory activities have been evaluated. The results of these biological assays showed that all of new derivatives are not endowed with improved anti-inflammatory activity against COX-1, but some of them showed a good activity against COX-2. To evaluate the binding mode of the most significative compounds (2d, 2f, 2g and 2k) docking studies were carried out. These studies confirmed biological data, in fact these compounds were able to fit into the active site of COX-2. (C) 2010 Elsevier Masson SAS. All rights reserved.
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收藏
页码：6135 / 6138
页数：4
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