Design, synthesis and molecular modeling study of acylated 1,2,4-triazole-3-acetates with potential anti-inflammatory activity

被引：99

作者：

Abdel-Megeed, Ashraf M. ^{[1
]}

Abdel-Rahman, Hamdy A. ^{[1
]}

Alkaramany, Gamal-Eldien S. ^{[1
]}

El-Gendy, Mahmoud A. ^{[1
]}

机构：

[1] Assiut Univ, Fac Pharm, Div Med Chem, Assiut 71526, Egypt

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 44卷 / 01期

关键词：

Heteroarylacetic acids; 1,2,4-Triazole; Acylation; Anti-inflammatory; Docking; COX-2; PHARMACOLOGICAL EVALUATION; ACID-DERIVATIVES; AGENTS; INHIBITORS; ANALOGS; ESTER;

D O I：

10.1016/j.ejmech.2008.03.017

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The present investigation is concerned with the synthesis of different acylated 1,2,4-triazole-3-acetates with the objective of discovering novel and potent anti-inflammatory agents. Structures of the synthesized compounds were elucidated by spectral and elemental analyses. The obtained compounds were evaluated for their anti-inflammatory activites as well as gastric ulcerogenic effects and acute toxicity. Results showed that 1-acylated-5-amino-1,2,4-triazole-3-acetates 3a-e showed higher anti-inflammatory activity than the corresponding 5-acylamino derivatives 4a-e in carageenan-induced rat paw edema test with low gastric ulcerogenicity compared with indomethacin. Furthermore, molecular modeling studies were performed in order to rationalize the obtained biological results. (C) 2008 Elsevier Masson SAS. All rights reserved.

引用

页码：117 / 123

页数：7

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