Synthesis and biological evaluation of novel HIV-1 protease inhibitors using tertiary amine as P2-ligands

被引：20

作者：

Yang, Zhi-Heng ^{[1
,2
]}

Bai, Xiao-Guang ^{[1
,2
]}

Zhou, Lei ^{[1
,2
]}

Wang, Ju-Xian ^{[1
,2
]}

Liu, Hong-Tao ^{[3
]}

Wang, Yu-Cheng ^{[1
,2
]}

机构：

[1] Chinese Acad Med Sci, Inst Med Biotechnol, Beijing 100050, Peoples R China

[2] Peking Union Med Coll, Beijing 100050, Peoples R China

[3] Hebei Gen Hosp, Dept Pharm, Shijiazhuang, Hebei, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2015年 / 25卷 / 09期

基金：

中国国家自然科学基金;

关键词：

HIV-1; protease; Inhibitors; HAART; Darunavir; STRUCTURE-BASED DESIGN; DRUG-RESISTANCE; INFECTED PATIENTS; THERAPY; MUTATIONS; RITONAVIR; LIGANDS;

D O I：

10.1016/j.bmcl.2015.03.047

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of tertiary amine derivatives exhibiting potent HIV-1 protease inhibiting properties were identified. These novel inhibitors were designed based on the structure of Darunavir with modification on the P2 and P2' position. This effort led to discovery of 35e and 38e, which exhibited excellent HIV-1 protease inhibition with IC50 values of 15 nM and 64 nM, respectively. (C) 2015 Elsevier Ltd. All rights reserved.

引用

页码：1880 / 1883

页数：4

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