Powers L J
J Med Chem. 1976 Jan;19(1):57-62. doi: 10.1021/jm00223a013.
Thirteen 2-methylbenzofurans were synthesized and their antibacterial activity was investigated. 2-Methyl-3-nitrobenzofuran and analogs containing 7-NO2, 5-NO2, 7-Br, 7-CONH2, and 7-CF3 substituents are bacteriostatic. The spectrum of activity of these compounds is similar to nitrofurazone; however, a strain of E. coli Br which has increased resistance to nitrofurazone did not show increased resistance to 3,7-dinitro-2-methylbenzofuran (1). The 3-nitro-2-methylbenzofurans are labile in solution (T1/2 0.8-3.5 hr at 37 degrees, pH 7.0). The solvolysis product of 1 was identified as alpha,6-dinitro-o-cresol (15). The 3-nitrobenzofurans are more potent in minimal media than in Penassay broth. This greater potency can be abolished by addition of casamino acids and tryptophan to the minimal media.
合成了13种2-甲基苯并呋喃，并研究了它们的抗菌活性。2-甲基-3-硝基苯并呋喃以及含有7-NO₂、5-NO₂、7-Br、7-CONH₂和7-CF₃取代基的类似物具有抑菌作用。这些化合物的活性谱与呋喃西林相似；然而，对呋喃西林耐药性增强的大肠杆菌Br菌株对3,7-二硝基-2-甲基苯并呋喃并未表现出耐药性增加（1）。3-硝基-2-甲基苯并呋喃在溶液中不稳定（在37℃、pH 7.0时半衰期为0.8 - 3.5小时）。1的溶剂解产物被鉴定为α,6-二硝基邻甲酚（15）。3-硝基苯并呋喃在基本培养基中比在检测肉汤中更有效。在基本培养基中添加酪蛋白氨基酸和色氨酸可消除这种更强的效力。
