Synthesis and Biological Evaluation of New Diarylpyrazole and Triarylimidazoline Derivatives as Selective COX-2 Inhibitors

被引：21

作者：

Abdellatif, Khaled R. A. ^{[1
,2
]}

Abdelgawad, Mohamed A. ^{[1
,3
]}

Labib, Madlen B. ^{[1
]}

Zidan, Taha H.

机构：

[1] Beni Suef Univ, Fac Pharm, Dept Organ Pharmaceut Chem, Bani Suwayf 62514, Egypt

[2] Ibn Sina Natl Coll Med Studies, Dept Pharmaceut Sci, Jeddah, Saudi Arabia

[3] Aljouf Univ, Coll Pharm, Dept Pharmaceut Chem, Sakaka, Aljouf, Saudi Arabia

来源：

ARCHIV DER PHARMAZIE | 2017年 / 350卷 / 08期

关键词：

Anti-inflammatory; Imidazoline; Pyrazole; Selective COX-2 inhibitor; DONOR ESTER PRODRUGS; ANTIINFLAMMATORY EVALUATION; CYCLOOXYGENASE INHIBITION; DESIGN;

D O I：

10.1002/ardp.201600386

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

New series of diarylpyrazoles 8a-f and triarylimidazoline-5-ones 11a-g were synthesized and evaluated for their in vitro cyclooxygenase-1 (COX-1) and COX-2 inhibitory activity and in vivo anti-inflammatory activity. The synthesized compounds showed good selectivity for COX-2; compounds 8a, 8d, 8f, 11a, and 11c exhibited the highest COX-2 selectivity indexes (SI=4.77-5.43) compared to the reference drug celecoxib (SI=7.8). All compounds showed good in vivo anti-inflammatory activity, especially compounds 8a, 8f, 11c, and 11d, which also showed some similarities to the time interval pattern of celecoxib at all different time intervals (1, 3, and 6h).

引用

页数：10

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