Design and synthesis of 3-pyrazolyl-thiophene, thieno[2,3-d]pyrimidines as new bioactive and pharmacological activities

被引：69

作者：

Hafez, H. N. ^{[1
]}

El-Gazzar, A. B. A. ^{[1
]}

机构：

[1] Natl Res Ctr, Photochem Dept, Heterocycl & Nucleoside Unit, Giza 12622, Egypt

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 19期

关键词：

3-pyrazolyl-thiophene; thieno[2,3-d]pyrimidines; antimicrobial; anti-inflammatory; analgesic; ulcerogenic activities;

D O I：

10.1016/j.bmcl.2008.08.071

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Two series of 5-ethyl-2-amino-3-pyrazolyl-4- methylthiophenecarboxylate and 2-thioxo-N-3-aminothieno[ 2,3-d]pyrimidines were prepared from 3,5-diethyl-2-amino-4-methylthio-phenecaboxylate and evaluated as anti-inflammatory, analgesic and ulcerogenic activities. Among the compounds studied, compounds which containing the substituted hydrazide at C-3 position 7, 16, and 17a showed more potent anti-inflammatory and analgesic activities than the standard drug (Indomethacin and Aspirin), along without ulcerogenity. While compounds 2, 5, 9, 10, and 11c showed moderate activities. Some of the newly synthesized compounds have good to excellent antimicrobial activity. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：5222 / 5227

页数：6

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