Novel 5-substituted 1H-tetrazoles as cyclooxygenase-2 (COX-2) inhibitors

被引：43

作者：

Al-Hourani, Baker Jawabrah ^{[1
,3
]}

Sharma, Sai Kiran ^{[1
,2
]}

Suresh, Mavanur ^{[2
]}

Wuest, Frank ^{[1
,2
]}

机构：

[1] Univ Alberta, Dept Oncol, Edmonton, AB, Canada

[2] Univ Alberta, Fac Pharm & Pharmaceut Sci, Edmonton, AB T6G 2N8, Canada

[3] Amer Univ Madaba, Fac Sci, Dept Chem, Madaba, Jordan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 06期

关键词：

Cyclooxygenase; COX-2; inhibitors; 5-Substituted; 1H-tetrazoles; PREVENTION; ENZYMES; CANCER;

D O I：

10.1016/j.bmcl.2012.01.093

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel 5-substituted 1H-tetrazoles as cyclooxygenase-2 (COX-2) inhibitors was prepared via treatment of various diaryl amides with tetrachlorosilane/sodium azide. All compounds were tested in cyclooxygenase (COX) assays in vitro to determine COX-1 and COX-2 inhibitory potency and selectivity. Tetrazoles contained a methylsulfonyl or sulfonamide group as COX-2 pharmacophore displayed only low inhibitory potency towards COX-2. Most potent compounds showed IC50 values of 6 and 7 mu M for COX-2. All compounds showed IC50 values greater 100 mu M for COX-1 inhibition. (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：2235 / 2238

页数：4

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