Abdel-Rahman Hamdy M, El-Koussi Nawal A, Hassan Hoda Y
Medicinal Chemistry Department, Faculty of Pharmacy, Assiut University, Assiut, Egypt.
Arch Pharm (Weinheim). 2009 Feb;342(2):94-9. doi: 10.1002/ardp.200800113.
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 microg/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 microg/mL concentration. At the same time, it proofed to be nontoxic to mammalian cells (IC(50) > 62.5 microg/mL in VERO cells).
设计并合成了一系列氟化的1,2,4-三唑并[1,5-a]嘧啶-6-羧酸衍生物作为氟喹诺酮类似物。以6.25微克/毫升的浓度针对结核分枝杆菌H(37)R(v)菌株对合成的化合物进行筛选。发现化合物4，即7-氧代-2-(三氟甲基)-4,7-二氢-1,2,4-三唑并[5,1-a]嘧啶-6-羧酸是一种非常有效的抑制剂，在6.25微克/毫升的浓度下能够抑制结核分枝杆菌H(37)R(v) 92%的生长。同时，它被证明对哺乳动物细胞无毒（在VERO细胞中的IC(50) > 62.5微克/毫升）。
