5,5-DISUBSTITUTED HYDANTOINS - SYNTHESES AND ANTI-HIV ACTIVITY

被引：68

作者：

COMBER, RN

REYNOLDS, RC

FRIEDRICH, JD

MANGUIKIAN, RA

BUCKHEIT, RW

TRUSS, JW

SHANNON, WM

SECRIST, JA

机构：

[1] Organic Chemistry Department, Southern Research Institute, Birmingham

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1992年 / 35卷 / 19期

关键词：

D O I：

10.1021/jm00097a014

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 5,5-disubstituted hydantoin derivatives was synthesized by alkylating 5,5-bis(mercaptomethyl)-2,4-imidazolidinedione (3) with various halomethylaromatic or halomethylheteroaromatic precursors, or by using the Buchener-Berg procedure on the required ketone. When evaluated for their ability to inhibit HIV-induced cell killing and virus production in CEM or MT-2 cells only compounds 2, 4n, 4o, and 4i demonstrated modest activity, the latter with an IC50 = 53-mu-M.

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页码：3567 / 3572

页数：6

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