Vigorita M G, Ottanà R, Zappalà C, Maccari R, Pizzimenti F C, Gabbrielli G
Dipartimenti Farmaco-chimico, Università di Messina, Italy.
Farmaco. 1995 Nov;50(11):783-6.
The 5-aryl-4-methyl-2-(4-pyridyl)-delta 2-1,3,4-oxadiazolines 3, previously synthesized along with isomer 4-aryl-1-methoxy-1-(4-pyridyl)-2,3-diaza-1,3-butadienes 2 from benzaldehyde isonicotinoylhydrazones and diazomethane, were tested for in vitro activity against both M. tuberculosis and some atypical mycobacterial strains as well as against human immunodeficiency virus (HIV-1). Some halophenyl derivatives, 3e, 3g, 3i, 3j, were found to display MIC ranges from 1 to 10 (micrograms/ml against H 37 Rv and a clinical isolate tubercular strain, whereas against M. avium (MAC) the MICs were higher than 20 micrograms/ml. When the combinations of oxadiazolines with ethambutol, acting as inhibitor of cell wall synthesis, were assayed on MAC strain a synergistic effect was demonstrated for 3g and 3h trifluoromethyl derivatives. The antimycobacterial profiles of 2 and 3 analogues are compared and discussed. As shown by compounds 2, no substantial anti-HIV in vitro activity was found in selected delta 2-oxadiazolines; a moderate cytotoxicity, however, appears to be a common property.
5-芳基-4-甲基-2-(4-吡啶基)-δ2-1,3,4-恶二唑啉3是之前由苯甲醛异烟酰腙和重氮甲烷与异构体4-芳基-1-甲氧基-1-(4-吡啶基)-2,3-二氮杂-1,3-丁二烯2一起合成的，对结核分枝杆菌和一些非典型分枝杆菌菌株以及人类免疫缺陷病毒(HIV-1)进行了体外活性测试。发现一些卤代苯基衍生物3e、3g、3i、3j对H 37 Rv和临床分离的结核菌株的最低抑菌浓度范围为1至10微克/毫升，而对鸟分枝杆菌(MAC)的最低抑菌浓度高于20微克/毫升。当在MAC菌株上测定恶二唑啉与作为细胞壁合成抑制剂的乙胺丁醇的组合时，证明3g和3h三氟甲基衍生物具有协同作用。对2和3类似物的抗分枝杆菌谱进行了比较和讨论。如化合物2所示，在选定的δ2-恶二唑啉中未发现实质性的体外抗HIV活性；然而，中等细胞毒性似乎是一个共同特性。
