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).
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页数：10
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