6-(3-FLUOROANILINO)-9-(SUBSTITUTED-BENZYL)-2-TRIFLUOROMETHYL-9H-PURINES WITH ANTIRHINOVIRUS ACTIVITY

被引：5

作者：

KELLEY, JL

LINN, JA

DAVIS, RG

SELWAY, JWT

机构：

[1] BURROUGHS WELLCOME CO, DIV ORGAN CHEM, RES TRIANGLE PK, NC 27709 USA

[2] WELLCOME RES LABS, BECKENHAM BR3 3BS, KENT, ENGLAND

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1990年 / 25卷 / 07期

关键词：

antiviral; benzylpurine; purine; rhinovirus; trifluoromethylpurine;

D O I：

10.1016/0223-5234(90)90188-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 6-(3-fluoroanilino)-9-(substituted-benzyl)-2-trifluoromethylpurines was synthesized and tested for antirhinovirus activity. Most of the compounds were prepared by alkylation of a 6-anilino-2-trifluoromethylpurine with a benzyl halide or by amination of a 6-chloro-9-benzylpurine with an aniline. Compounds with a variety of para-benzyl substituents had activity against rhinovirus serotype 1B. The 6-(3-fluoroanilino)-9-(3-fluorobenzyl)-2-trifluoromethylpurine 15 had good activity (IC50s = 0.4-13 μM) against 80% of the 47 serotypes tested, but pharmacokinetic studies indicated poor oral bioavailability. © 1990.

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页码：623 / 628

页数：6

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