Synthesis of some novel 2-substituted-5-[isopropylthiazole] clubbed 1,2,4-triazole and 1,3,4-oxadiazoles as potential antimicrobial and antitubercular agents

被引：191

作者：

Kumar, G. V. Suresh ^{[1
]}

Rajendraprasad, Y. ^{[2
]}

Mallikarjuna, B. P. ^{[3
]}

Chandrashekar, S. M. ^{[1
]}

Kistayya, C. ^{[2
]}

机构：

[1] St Johns Pharm Coll, Dept Med Chem, Bangalore 560040, Karnataka, India

[2] Andhra Univ, Dept Pharmaceut Sci, Visakhapatnam 530003, Andhra Pradesh, India

[3] PES Coll Pharm, Dept Med Chem, Bangalore 560050, Karnataka, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 45卷 / 05期

关键词：

4-Isopropylthiazole-2-carbohydrazide analogs; Clubbed triazole-thiazole derivatives; Cytotoxicity; Antibacterial; Antifungal; Antitubercular; Broth dilution assay; MICROWAVE-ASSISTED SYNTHESIS; DERIVATIVES; BIOSYNTHESIS; MYCOBACTERIA; TRIAZOLES; SYSTEMS; GROWTH;

D O I：

10.1016/j.ejmech.2010.01.045

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In the present study a series of 2-substituted-5-[isopropylthiazole] clubbed 1,2,4-triazole and 1,3,4-oxadiazole derivatives have been synthesized and characterized by IR, (1)H NMR, (13)C NMR and mass spectral analysis. Synthesized compounds were evaluated for their preliminary cytotoxicity, antimicrobial and antitubercular activity against Mycobacterium tuberculosis H37Rv strain by broth dilution assay method. Antimycobacterial activity tested against M. tuberculosis indicated that compounds 4b and 6g exhibited twofold enhanced potency than parent compound 1 and the results indicate that some of them exhibited promising activities and they deserve more consideration as potential antitubercular agents. Compound 3c, 4b and 6c exhibited good or moderate antibacterial inhibition and compounds 3h and 7c showed excellent antifungal activity. (C) 2010 Elsevier Masson SAS. All rights reserved.

引用

页码：2063 / 2074

页数：12

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