SYNTHESIS AND ANTIRHINOVIRUS ACTIVITY OF 8-SUBSTITUTED ANALOGS OF 6-(DIMETHYLAMINO)-9-(4-METHYLBENZYL)-2-(TRIFLUOROMETHYL)-9H-PURINE

被引:16
作者
KELLEY, JL [1 ]
LINN, JA [1 ]
SELWAY, JWT [1 ]
机构
[1] WELLCOME RES LABS,BECKENHAM BR3 3BS,KENT,ENGLAND
关键词
D O I
10.1021/jm00105a023
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Several 8-substituted analogues of 6-(dimethylamino)-9-(4-methylbenzyl)-2-(trifluoromethyl)-9H-purine (1) were synthesized and tested for activity against rhinovirus type 1B. Among 16 8-substituted analogues, the 8-amino (3) and 8-bromo (2) analogues were most active with IC50s of 0.36 and 1.4-mu-M, respectively, under conditions where 1 had an IC50 of 0.03-mu-M.
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页码:157 / 160
页数:4
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