NOVEL AZOLYLALKYLOXY COMPOUNDS WITH ANTIPICORNAVIRAL ACTIVITY

被引:4
作者
ABEL, MD [1 ]
CAMERON, AD [1 ]
HA, CM [1 ]
KOSKI, CA [1 ]
LUU, HT [1 ]
MICETICH, RG [1 ]
NGUYEN, DQ [1 ]
TEMPEST, ML [1 ]
DANESHTALAB, M [1 ]
机构
[1] SYNPHAR LABS INC,EDMONTON,AB T6E 5V2,CANADA
关键词
AZOLYLALKYLOXY COMPOUNDS; ENTEROVIRUS; PICORNAVIRUS; RHINOVIRUS;
D O I
10.1177/095632029500600407
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
A novel series of azolylalkyloxy compounds was designed, synthesized and evaluated for antipicornaviral activity. Several of the compounds exhibited in vitro activity comparable to that of Disoxaril. An investigation of qualitative structure-activity relationships indicated that the optimal length of the alkyl chain is six or seven carbon atoms, with seven being marginally superior. The effect of different azole moieties on activity was relatively small, with 3-methylisoxazole and 4-methylthiazole being most effective. The nature of the oxy substituent was found to be extremely important for antipicornaviral activity. The 2-dibenzofuryl group proved to be the most effective oxy substituent for this class of compounds. Compounds 11 and 22, combining dibenzofuran with 3-methylisoxazole and 4-methylthiazole, respectively, were highly effective in vitro against a wide range of human rhinoviruses as well as several enteroviruses.
引用
收藏
页码:245 / 254
页数:10
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