Arena A, Capozza A B, Maccari R, Ottanà R, Vigorita M G
Instituto di Microbiologia, Facoltà di Medicina e Chirurgia, Università di Messina, Italy.
Farmaco. 1996 Jul;51(7):517-23.
The synthesis and evaluation of antiviral in vitro activity are reported of some 2'-(1-arylethyl)isonicotinohydrazides (5a-d) and N-(1-arylethyl)isonicotinohydrazonic acids (6a-d), obtained by reducing fluorinated acetophenone isonicotinoylhydrazones (2a-d) with sodium cyanoborohydride. These INH analogues, along with other ones previously prepared, i.e. benzaldehyde isonicotinoylhydrazones 1, 4-aryl-1-methoxyl-1-(4-pyridyl)-2,3-diaza-1,3-butadienes 3 and 5-aryl-4-methyl-2-(4-pyridyl)-delta 2-1,3,4-oxadiazolines 4, were assayed for anti-HSV-1 activity on the monoblastoid cell line U937. Only some compounds (1b, 1d, 4d and 4e) displayed a moderate antiherpetic activity. In addition, the reduced compounds 5 and 6, submitted to the anti-HIV-1 screening, did not display significant effects in reducing virus-induced cytopathogenicity. The cytotoxicity of all compounds has been assayed on Vero cells and some considerations in correlation with structure are discussed.
报道了通过用氰基硼氢化钠还原氟化苯乙酮异烟酰腙（2a - d）得到的一些2'-（1 - 芳基乙基）异烟酰肼（5a - d）和N - （1 - 芳基乙基）异烟酰腙酸（6a - d）的合成及其体外抗病毒活性评价。这些异烟肼类似物，连同先前制备的其他类似物，即苯甲醛异烟酰腙1、4 - 芳基 - 1 - 甲氧基 - 1 - （4 - 吡啶基） - 2,3 - 二氮杂 - 1,3 - 丁二烯3和5 - 芳基 - 4 - 甲基 - 2 - （4 - 吡啶基） - δ2 - 1,3,4 - 恶二唑啉4，在单核细胞样细胞系U937上测定了抗HSV - 1活性。只有一些化合物（1b、1d、4d和4e）表现出中等抗疱疹活性。此外，对还原产物5和6进行抗HIV - 1筛选时，它们在降低病毒诱导的细胞病变效应方面未显示出显著效果。已在Vero细胞上测定了所有化合物的细胞毒性，并讨论了与结构相关的一些考虑因素。
