Synthesis and biological evaluation of novel substituted 1,3,4-thiadiazole and 2,6-di aryl substituted imidazo [2,1-b] [1,3,4] thiadiazole derivatives

被引：60

作者：

Chandrakantha, B. ^{[1
]}

Isloor, Arun M. ^{[2
]}

Shetty, Prakash ^{[3
]}

Fun, Hoong Kun ^{[4
]}

Hegde, Gurumurthy ^{[5
]}

机构：

[1] Manipal Univ, Dept Chem, Manipal Inst Technol, Manipal 576104, Karnataka, India

[2] Natl Inst Technol Karnataka, Med Chem Lab, Dept Chem, Mangalore 575025, Karnataka, India

[3] Manipal Univ, Manipal Inst Technol, Dept Printing & Media Engn, Manipal 576104, Karnataka, India

[4] King Saud Univ, Coll Pharm, Dept Pharmaceut Chem, Riyadh 11451, Saudi Arabia

[5] Univ Malaysia Pahang, Fac Ind Sci & Technol, Kuantan 26300, Pahang Darul Ma, Malaysia

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2014年 / 71卷

关键词：

1,3,4-Thiadiazole; 2,6-Diaryl imidazo [2,1-b] [1,3,4] thiadiazole; Antibacterial; Antifungal activity; ANTIBACTERIAL ACTIVITY; ANTIVIRAL ACTIVITY; IN-VITRO; ANTITUMOR;

D O I：

10.1016/j.ejmech.2013.10.056

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new series of N-[5-(4-(alkyl/aryl)-3-nitro-phenyl)-[1,3,4-thiadiazol-2-yl]-2,2-dimethyl-propionamide 4 (a-1) and 6-(4-Methoxy-phenyl)-2-(4-alkyl/aryl)-3-nitro-phenyl)-Imidazo [2,1-b] [1,3,4] thiadiazole 6 (a-1) were synthesized starting from 5-(4-Fluoro-3-nitro-phenyl)-[1,3,4] thiadiazole-2-ylamine. The synthesized compounds were characterized by IR, NMR, mass spectral and elemental analysis. All the compounds were tested for antibacterial and antifungal activities. The antimicrobial activities of the compounds were assessed by well plate method (zone of inhibition). Compounds 4a, 4c and 6e, 6g displayed appreciable activity at the concentration 0.5-1.0 mg/mL. (C) 2013 Elsevier Masson SAS. All rights reserved.

引用

页码：316 / 323

页数：8

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