Premium
Fluorinated 1,2,4‐Triazolo[1,5‐ a ]pyrimidine‐6‐carboxylic Acid Derivatives as Antimycobacterial Agents
Author(s) -
AbdelRahman Hamdy M.,
ElKoussi Nawal A.,
Hassan Hoda Y.
Publication year - 2009
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200800113
Subject(s) - antimycobacterial , pyrimidine , carboxylic acid , chemistry , vero cell , mycobacterium tuberculosis , stereochemistry , trifluoromethyl , antibacterial agent , tuberculosis , antibiotics , organic chemistry , in vitro , biochemistry , medicine , alkyl , pathology
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 μg/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 μg/mL concentration. At the same time, it proofed to be nontoxic to mammalian cells (IC 50 > 62.5 μg/mL in VERO cells).