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Synthesis and antirhinovirus activity of 8-substituted analogues of 6-(dimethylamino)-9-(4-methylbenzyl)-2-(trifluoromethyl)-9H-purine.

作者信息

Kelley J L, Linn J A, Selway J W

机构信息

Division of Organic Chemistry, Burroughs Wellcome Co., Research Triangle Park, North Carolina 27709.

出版信息

J Med Chem. 1991 Jan;34(1):157-60. doi: 10.1021/jm00105a023.

Abstract

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 microM, respectively, under conditions where 1 had an IC50 of 0.03 microM.

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