Synthesis and biological evaluation of quinolines, thiazolo[3,2-a]pyrimidines, thiadiazolo[3,2-a]pyrimidines and triazolo[3,4-b][1,3,4]thiadiazepines as antimicrobial agents

被引：10

作者：

Sahi, Seema ^{[1
]}

Paul, Satya ^{[1
]}

机构：

[1] Univ Jammu, Dept Chem, Jammu 180006, India

来源：

MEDICINAL CHEMISTRY RESEARCH | 2016年 / 25卷 / 05期

关键词：

Quinolines; Thiazolo[3,2-a]pyrimidines; Thiadiazolo[3,2-a]pyrimidines; Triazolo[3,4-b][1,3,4]thiadiazepines; 3-Triazolylthioacetic acid; Organocatalyst; MICROWAVE; ORGANOCATALYST; CONDENSATION; DERIVATIVES;

D O I：

10.1007/s00044-016-1540-z

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Series of quinolines, thiazolo[3,2-a]pyrimidines, thiadiazolo[3,2-a]pyrimidines and triazolo[3,4-b][1,3,4]thiadiazepines were synthesized by the reaction of amino compound, aromatic aldehyde and malononitrile/ethyl cyanoacetate, using 2-[5-(4-methoxyphenyl)-4H-1,2,4-triazol-3-ylthio]acetic acid as an organocatalyst in water-ethanol mixture. Synthesized compounds were evaluated for in vitro antibacterial and antifungal activities against three fungal and five bacterial strains. Some of them exhibited good activity in comparison with the standard fluconazole and streptomycin such as compound 16h has shown best antifungal activity with MIC value of 60 A mu g/mL against A. niger and 12g exhibited best antibacterial activity with MIC value of 50 A mu g/mL against E. coli.

引用

页码：951 / 969

页数：19

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