Synthesis of (+)-biotin derivatives as HIV-1 protease inhibitors

被引：3

作者：

Han, Q

Lafontaine, J

Bacheler, LT

Rayner, MM

Klabe, RM

EricksonViitanen, S

Lam, PYS

机构：

[1] Chemical and Physical Sciences, The DuPont Merck Pharmaceutical Co., Experimental Station, Wilmington, DE 19880-0500

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 12期

关键词：

D O I：

10.1016/0960-894X(96)00233-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Several bis-N-alkylated (+)-biotin derivatives were synthesized and evaluated for activities against HIV-1 protease. The most potent inhibitor, 2D, synthesized in two steps from (+)-biotin, has K-i of 0.50 mu M and antiviral IC90 of 7 mu M. The (+)-biotin analogs in general have good translations from enzymatic K-i to antiviral cell assay IC90. Copyright (C) 1996 Elsevier Science Ltd

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页码：1371 / 1374

页数：4

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