Synthesis and pharmacological evaluation of newer thiazolo [3,2-a] pyrimidines for anti-inflammatory and antinociceptive activity

被引：53

作者：

Alam, Ozair ^{[1
]}

Khan, Suroor A. ^{[1
]}

Siddiqui, Nadeem ^{[1
]}

Ahsan, Waquar ^{[1
]}

机构：

[1] Hamdard Univ, Dept Pharmaceut Chem, Fac Pharm, New Delhi 110062, India

来源：

MEDICINAL CHEMISTRY RESEARCH | 2010年 / 19卷 / 09期

关键词：

Thiazolopyrimidine; Anti-inflammatory; Antinociceptive; Acute toxicity; ADENOSINE KINASE INHIBITOR; AGENTS; DERIVATIVES; RAT;

D O I：

10.1007/s00044-009-9267-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new series of thiazolo [3,2-a] pyrimidine derivatives was designed and synthesized using 4-fluoroaniline and ethylacetoacetate as starting material. Anti-inflammatory activity was assessed by the rat paw edema method and antinociceptive activity was evaluated by thermal stimulus technique. The compounds 5-(4-chlorophenyl)-2-(4-fluorobenzylidene)-7-methyl-3-oxo-2,3-dihydro-5H-thiazolo[3,2-a]pyrimidine-6-carboxylic acid (4-fluorophenyl)amide (3l) and 2-(4-chlorobenzylidene)-5-(4-fluorophenyl)-7-methyl-3-oxo-2,3-dihydro-5H-thiazolo[3,2-a]pyrimidine-6-carboxylic acid (4-fluorophenyl)amide (3q) were found to possess significant anti-inflammatory and antinociceptive activities. These compounds also showed lower ulcerogenic activity and higher ALD(50) values. Compounds with an aryl ring substituted with a smaller electron withdrawing group at the fourth position displayed better activity than the other derivatives.

引用

页码：1245 / 1258

页数：14

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