Nonpeptidic HIV protease inhibitors:: 6-alkyl-5,6-dihydropyran-2-ones possessing a novel and achiral 3-(2-t-butyl-5-methyl-4-sulfamate)phenylthio moiety.

被引：6

作者：

Prasad, JVNV

Markoski, LJ

Boyer, FE

Domagala, JM

Ellsworth, EL

Gajda, C

Hagen, SE

Tait, BD

Lunney, EA

Tummino, PJ

Ferguson, D

Holler, T

Hupe, D

Nouhan, C

Gracheck, SJ

VanderRoest, S

Saunders, J

Iyer, K

Sinz, M

机构：

[1] Parke Davis Pharmaceut Res, Div Warner Lambert Co, Dept Chem, Ann Arbor, MI 48106 USA

[2] Parke Davis Pharmaceut Res, Div Warner Lambert Co, Dept Biochem, Ann Arbor, MI 48106 USA

[3] Parke Davis Pharmaceut Res, Div Warner Lambert Co, Dept Infect Dis, Ann Arbor, MI 48106 USA

[4] Parke Davis Pharmaceut Res, Div Warner Lambert Co, Dept PDM, Ann Arbor, MI 48106 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 15期

关键词：

D O I：

10.1016/S0960-894X(99)00360-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Dihydropyran-Zones possessing a sulfamate moiety at the 4-position of the thiophenyl ring were designed to reach S-3' pocket of the HIV protease. Synthetic routes for the preparation of thiotosylates possessing 3-(2-t-butyl-5-methyl-4-sulfamate) phenylthio moiety were established. SAR of various sulfamate analogs including HIV protease binding affinities, antiviral activities and therapeutic indices will be described. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：2217 / 2222

页数：6

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