RATIONAL DESIGN OF IRREVERSIBLE, PSEUDO-C-2-SYMMETRICAL HIV-1 PROTEASE INHIBITORS

被引：20

作者：

PARK, CH ^{[1
]}

KOH, JS ^{[1
]}

SON, YC ^{[1
]}

CHOI, HI ^{[1
]}

LEE, CS ^{[1
]}

CHOY, NY ^{[1
]}

MOON, KY ^{[1
]}

JUNG, WH ^{[1
]}

KIM, SC ^{[1
]}

YOON, HS ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 16期

关键词：

D O I：

10.1016/0960-894X(95)00306-E

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Pseudo-C-2-symmetric irreversible inhibitors of HIV-1 protease containing cis-epoxide were designed, synthesized, and kinetically characterized. Introduction of a Gly residue into P-1' of the inactivators yielded strong time-dependent irreversible ones with k(ina)/K-i ranging from 1.5x10(8) to 3.4x10(5) M(-1) min(-1).

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页码：1843 / 1848

页数：6

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