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早期关于苯骈咪唑抑制病毒增殖的报告,促进了对多种苯骈咪唑类似物的研究。发现2-(α-羟苄基)苯骈咪唑(HBB)对病毒的特异性作用以及(S,S)-1,2-双(5-甲氧基-2-苯骈咪唑)-1,2-乙二醇在组织培养和黑猩猩试验中是病毒增殖的良好抑制剂。本文报道(4)和(5)顺、反异构体的合成、分离及抗病毒研究。(4)与(5)的结构是由~(13)CNMR 谱及(5)的 X-射线衍射分析确定。两者对15种不同血清型鼻病毒的增殖均有显著的抑制作用。但作为鼻病毒抑制剂,反式异构体(5)比顺式异构体(4)活性更大。作者认为1,2,6位取代基是必要的活性基团。两者具有广谱特异性抗病毒作用。在小鼠与狗的试验中口服血药浓度与肺部浓度高于 ID_(50)值,在鼻
Early reports of benzodiazepines on the inhibition of virus proliferation facilitated the study of a variety of benzimidazole analogs. The specific effect of 2- (α-hydroxybenzyl) benzimidazole (HBB) on viruses and the effect of (S, S) -1,2- bis (5-methoxy-2-benzimidazole) 2-Ethylene glycol is a good inhibitor of virus proliferation in tissue culture and chimpanzee assays. This paper reports (4) and (5) cis, trans isomer synthesis, isolation and antiviral studies. The structures of (4) and (5) are determined by ~ (13) CNMR spectra and X-ray diffraction analysis of (5). Both of the 15 different serotypes of rhinovirus proliferation were significantly inhibited. However, as a rhinovirus inhibitor, trans isomer (5) is more active than cis isomer (4). The authors consider the 1,2,6 substituent is an essential active group. Both have a broad spectrum of specific antiviral effects. In mice and dogs in the test oral plasma concentration and lung concentration higher than the ID50 value in the nose