Design of a series of bicyclic HIV-1 integrase inhibitors. Part 1: Selection of the scaffold

被引：36

作者：

Jones, Eric D. ^{[1
]}

Vandegraaff, Nick ^{[1
]}

Le, Giang ^{[1
]}

Choi, Neil ^{[1
]}

Issa, William ^{[1
]}

Macfarlane, Katherine ^{[1
]}

Thienthong, Neeranat ^{[1
]}

Winfield, Lisa J. ^{[1
]}

Coates, Jonathan A. V. ^{[1
]}

Lu, Long ^{[2
]}

Li, Xinming ^{[2
]}

Feng, Xiao ^{[2
]}

Yu, Changjiang ^{[2
]}

Rhodes, David I. ^{[1
]}

Deadman, John J. ^{[1
]}

机构：

[1] Avexa Ltd, Richmond, Vic 3121, Australia

[2] Chinese Acad Sci, Shanghai Inst Organ Chem, Shanghai 200032, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 19期

关键词：

Integrase; Inhibitor; Synthesis; 3-Hydroxy-pyrido[12-a]pyrimidin-4-one;

D O I：

10.1016/j.bmcl.2010.07.079

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

HIV integrase inhibitors based on a novel bicyclic pyrimidinone core is presented. Nine variations of the core scaffold are evaluated leading to optimization of the 6:6 core giving compound 48 with an EC50 of 3 nM against wild type HIV infected T-cells. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：5913 / 5917

页数：5

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