Design and synthesis of pyridin-2-yloxymethylpiperidin-1-ylbutyl amide CCR5 antagonists that are potent inhibitors of M-tropic (R5) HIV-1 replication

被引：9

作者：

Skerlj, Renato ^{[1
]}

Bridger, Gary ^{[2
]}

Zhou, Yuanxi ^{[2
]}

Bourque, Elyse ^{[1
]}

Langille, Jonathan ^{[2
]}

Di Fluri, Maria ^{[2
]}

Bogucki, David ^{[2
]}

Yang, Wen ^{[2
]}

Li, Tongshuang ^{[2
]}

Wang, Letian ^{[2
]}

Nan, Susan ^{[2
]}

Baird, Ian ^{[2
]}

Metz, Markus ^{[1
]}

Darkes, Marilyn ^{[2
]}

Labrecque, Jean ^{[2
]}

Lau, Gloria ^{[1
]}

Fricker, Simon ^{[1
]}

Huskens, Dana ^{[3
]}

Schols, Dominique ^{[3
]}

机构：

[1] Genzyme Corp, Waltham, MA 02451 USA

[2] AnorMED Inc, Langley, BC V2Y 1N5, Canada

[3] Katholieke Univ Leuven, Rega Inst Med Res, B-3000 Louvain, Belgium

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 08期

关键词：

CCR5; Chemokine receptor; HIV-1; Schering C; IMMUNODEFICIENCY-VIRUS TYPE-1; BIOLOGICAL EVALUATION; RECEPTOR; MARAVIROC; AMD3100;

D O I：

10.1016/j.bmcl.2011.02.058

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of CCR5 antagonists were identified based on the redesign of Schering C. An SAR was established based on inhibition of CCR5 (RANTES) binding and these compounds exhibited potent inhibition of R5 HIV-1 replication in peripheral blood mononuclear cells. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：2450 / 2455

页数：6

共 34 条

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