关键词:
Science
Humanities and Social Sciences
multidisciplinary
摘要:
THE antiviral activity of 2-(a-hydroxybenzyl)-benz-imidazole (HBB) (I: R = H) was first reported by Hollinshead and Smith1. Tamm et al.2 carried out a survey of the activities of promising benzimidazoles and benzotriazoles towards type 2 poliovirus and concluded that HBB and its 6-chloro derivative possessed greater selective action than other compounds studied and that these two had clinical potentialities. O5 Sullivan and Sadler3 showed that marked activity was also possessed by 2-(o-hydroxybenzyl)-benzimidazole, but that the corresponding p-hydroxybenzyl derivative was inactive. "Further work in this laboratory has involved synthesizing and testing, in tissue-culture, compounds structurally related to HBB. These include N-substituted derivatives (I), compounds substituted at the a-carbon atom (II), 2-benzoylbenzimidazole (III) and its derivatives, derivatives with a substituent in a benzene ring (IV), bisbenzimidazoles (V), benzimidazoHum salts and optical enantiomorphs of the above. The last two classes, both containing compounds with marked protective action against poliovirus, are to be discussed in subsequent publications. Meanwhile, the recent paper by Wagner, Wittreich, Lusi and Folkers4 describing the preparation of a number of compounds related to HBB for antiviral investigations makes this early publication of some of our findings ***. 1. Lines obtained in assay of protection given by HBB and its 1-alkyl derivatives against cytopathic effects of poliovirus type 1. (1) Control line (test-compounds absent) (circles); (2) HBB (100 ^M) (squares); (3) 1-Methyl derivative (80,uM) (dots); (4) 1-Ethyl derivative (80,wM) (crosses); (5) 1-Propyl derivative (40 ^M); (6) 1-Butyl derivative (20 /uM) (triangles). Line I also represents the control line when concentrations in column Y (Table 1) were used in an assay and line 2 corresponds closely to the lines obtained for HBB and its 1-alkyl derivatives in these concentrations. Regions a,p,y,d and e indicate