Synthesis of novel 1,3,4-trisubstituted pyrazoles as anti-inflammatory and analgesic agents

被引：92

作者：

Ragab, Fatma A. ^{[1
]}

Gawad, Nagwa M. Abdel ^{[1
]}

Georgey, Hanan H. ^{[1
]}

Said, Mona F. ^{[1
]}

机构：

[1] Cairo Univ, Fac Pharm, Dept Pharmaceut Chem, Cairo, Egypt

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2013年 / 63卷

关键词：

Pyrazole; Schiff's base; Pyrrole; Anti-inflammatory; Analgesic; COX inhibition; SELECTIVE COX-2 INHIBITORS; BIOLOGICAL EVALUATION; CYCLOOXYGENASE-2; INHIBITORS; DERIVATIVES; DESIGN; SYNTHASE; ASPIRIN; DRUGS; ACIDS; RAT;

D O I：

10.1016/j.ejmech.2013.03.005

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Some novel 1,3,4-trisubstituted pyrazoles were synthesized and screened for their anti-inflammatory and analgesic activities as well as their ulcerogenic liability. They showed anti-inflammatory and analgesic activities with better GIT tolerance than the standard drug phenylbutazone. In addition, IC50 values for 5e and 8e were recorded. Compound 5e was found to be the most active one as anti-inflammatory and analgesic agent. On the other hand, COX-1/COX-2 isozyme selectivity was also done which showed equal inhibition to both isoforms. (c) 2013 Elsevier Masson SAS. All rights reserved.

引用

页码：645 / 654

页数：10

共 40 条

[21]

MEADE EA, 1993, J BIOL CHEM, V268, P6610

[22]

Meshali M., 1983, Acta Pharm. Technol., V29, P217

[23]

OKUN R, 1963, J PHARMACOL EXP THER, V139, P107

[24]

Okunrobo Lucky O, 2006, Acta Pol Pharm, V63, P25

[25]

Paal C., 1884, Ber, V17, P2756, DOI [DOI 10.1002/CBER.188401702228, 10.1002/cber.188401702228]

[26] Synthesis of Novel Indolyl-Pyrimidine Antiinflammatory, Antioxidant and Antibacterial Agents [J].

Panda, S. S. ;

Chowdary, P. V. R. .

INDIAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2008, 70 (02) :208-215

[27] Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: Identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide (SC-58635, Celecoxib) [J].

Penning, TD ;

Talley, JJ ;

Bertenshaw, SR ;

Carter, JS ;

Collins, PW ;

Docter, S ;

Graneto, MJ ;

Lee, LF ;

Malecha, JW ;

Miyashiro, JM ;

Rogers, RS ;

Rogier, DJ ;

Yu, SS ;

Anderson, GD ;

Burton, EG ;

Cogburn, JN ;

Gregory, SA ;

Koboldt, CM ;

Perkins, WE ;

Seibert, K ;

Veenhuizen, AW ;

Zhang, YY ;

Isakson, PC .

JOURNAL OF MEDICINAL CHEMISTRY, 1997, 40 (09) :1347-1365

[28] Synthesis and antiinflammatory activity of some new 1,3,5-trisubstituted pyrazolines bearing benzene sulfonamide [J].

Rathish, I. G. ;

Javed, Kalim ;

Ahmad, Shamim ;

Bano, Sameena ;

Alam, M. S. ;

Pillai, K. K. ;

Singh, Surender ;

Bagchi, Vivek .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2009, 19 (01) :255-258

[29]

ROBERT A, 1968, GASTROENTEROLOGY, V55, P481

[30]

Schmidt J.G., 1881, BER DTSCH CHEM GES, V14, P1459, DOI [10.1002/cber.188101401306, DOI 10.1002/CBER.188101401306]

← 1 2 3 4 →