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

被引：32
|
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
收藏
页码：94 / 99
页数：6
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