Nardi D, Massarani E, Tajana A, Cappelletti R, Salvaterra M
Farmaco Sci. 1975 Apr;30(4):248-59.
A series of 2-methyldialkylammoniumalkylthio-4,p-substituted phenyl-3H-1,5-benzodiazepine iodides has been synthesized. Some compounds showed high selective activity against Staph. aureus and Strep. pyogenes. The nature of the sustituents at the phenyl moiety bound to the 4-position of the 1,5-benzodiazepine ring is of decisive influence, wherease the length of the aliphatic chain and the modification of the cationic head are of minor importance for the activity. The most active compound, 2-methyldiethylammoniumethylthio-4,p-phenylthiophenyl-3H-1,5-benzodiazepine iodide (XXXVIII), was selected for further research.
合成了一系列2-甲基二烷基铵烷基硫代-4，对取代苯基-3H-1，5-苯并二氮杂碘化物。一些化合物对金黄色葡萄球菌和化脓性链球菌表现出高选择性活性。与1，5-苯并二氮杂环4位相连的苯基部分取代基的性质具有决定性影响，而脂肪族链的长度和阳离子头部的修饰对活性影响较小。选择最具活性的化合物2-甲基二乙铵乙硫基-4，对苯硫基苯基-3H-1，5-苯并二氮杂碘化物（XXXVIII）进行进一步研究。
