SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF ANTIINFLAMMATORY 1-METHYL-2-(4-X-BENZOYL)IMIDAZOLE-5-ACETIC ACIDS

被引：8
作者：
CALIENDO, G
CIRINO, G
GRECO, G
NOVELLINO, E
PERISSUTTI, E
PINTO, A
SANTAGADA, V
SILIPO, C
SORRENTINO, L
机构：
[1] UNIV NAPLES FEDERICO II, DIPARTIMENTO CHIM FARMACEUT & TOSSICOL, I-80131 NAPLES, ITALY
[2] UNIV NAPLES FEDERICO II, DIPARTIMENTO FARMACOL SPERIMENTALE, I-80131 NAPLES, ITALY
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1994年 / 29卷 / 05期
关键词：
IMIDAZOLE; ANALGESIC-ANTIINFLAMMATORY ACTIVITY; CYCLOOXYGENASE; SAR;
D O I：
10.1016/0223-5234(94)90063-9
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A set of 1-methyl-2-(4-X-benzoyl)imidazole-5 acetic acids that are structurally related to tolmetin and zomepirac were synthesized and biologically evaluated for their antiinflammatory activity. The results of in vivo tests and enzymatic assays showed that some of the investigated compounds are characterized by an analgesic-antiinflammatory profile similar or better than that of tolmetin. Preliminary structure-activity relationships suggest that activity is promoted by electron-releasing substituents in the para-position of the benzoyl moiety.
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收藏
页码：381 / 388
页数：8
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