Fluorinated 1,2,4-Triazolo[1,5-a]pyrimidine-6-carboxylic Acid Derivatives as Antimycobacterial Agents

被引：33

作者：

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

El-Koussi, Nawal A. ^{[1
]}

Hassan, Hoda Y. ^{[1
]}

机构：

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

来源：

ARCHIV DER PHARMAZIE | 2009年 / 342卷 / 02期

关键词：

Antimycobacterial activity; Fluoroquinolone analogues; Mycobacterium tuberculosis; 1,2,4-Triazolo[1,5-a]pyrimidines; POTENTIAL ANTIMICROBIAL AGENTS; ANTIBACTERIAL ACTIVITY; MYCOBACTERIUM-TUBERCULOSIS; QUINOLONE ANTIBACTERIALS; ANALOGS;

D O I：

10.1002/ardp.200800113

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of fluorinated 1,2,4-triazolo[1,5-a]pyrimidine-6-carboxylic acid derivatives was designed and synthesized as fluoroquinolone analogues. The synthesized compounds were screened against Mycobacterium tuberculosis H(37)R(v) strain at 6.25 mu g/mL concentration. Compound 4, the 7-oxo-2-(trifluoromethyl)-4,7-dihydro-1,2,4-triazolo[5,1-a]pyrimidine-6-carboxylic acid was found to be a very potent inhibitor, being able to inhibit 92% growth of M. tuberculosis H(37)R(v) at 6.25 mu g/mL concentration. At the same time, it proofed to be nontoxic to mammalian cells (IC(50) > 62.5 mu g/mL in VERO cells).

引用

页码：94 / 99

页数：6

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