Synthesis of irreversible HIV-1 protease inhibitors containing sulfonamide and sulfone as amide bond isosteres

被引：28

作者：

Choy, N ^{[1
]}

Choi, HI ^{[1
]}

Jung, WH ^{[1
]}

Kim, CR ^{[1
]}

Yoon, H ^{[1
]}

Kim, SC ^{[1
]}

Lee, TG ^{[1
]}

Koh, JS ^{[1
]}

机构：

[1] LG CHEM LTD,BIOTECH RES INST,TAEJON 305380,SOUTH KOREA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 20期

关键词：

D O I：

10.1016/S0960-894X(97)10054-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Novel irreversible HIV-1 protease inhibitors containing sulfonamide and sulfone as amide bond isosteres were designed, synthesized, and kinetically characterized, A representative compound 2 displayed rapid, time-dependent inactivation of HIV-1 protease and high potency in cell culture with IC50 of 6.6 nM. (C) 1997 Published by Elsevier Science Ltd.

引用

页码：2635 / 2638

页数：4

共 15 条

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