Structural Modifications of DAPY Analogues with Potent Anti-HIV-1 Activity

✍ Scribed by Xiao-Qing Feng; Yong-Hong Liang; Zhao-Sen Zeng; Fen-Er Chen; Jan Balzarini; Christophe Pannecouque; Erik De Clercq

• Publisher: John Wiley and Sons
• Year: 2009
• Tongue: English
• Weight: 284 KB
• Volume: 4
• Category: Article
• ISSN: 1860-7179
• DOI: 10.1002/cmdc.200800334

✦ Synopsis

Abstract

A novel series of diarylpyrimidine analogues (DAPYs) featuring a naphthyl moiety at the C4 position were designed, with all compounds exhibiting strong activity against wild‐type HIV‐1.magnified image

A novel series of diarylpyrimidine analogues (DAPYs) featuring a naphthyl moiety at the C4 position were synthesized and evaluated for their in vitro activity against HIV in MT‐4 cells. All compounds exhibited strong activity against wild‐type HIV‐1. The most active compound showed activity against wild‐type HIV‐1 with an EC~50~ value of 2.35 nM and against the double mutant strain (K103N+Y181C) with an EC~50~ value of 6.6 μM, with a selectivity index greater than 60 000 against wild‐type HIV‐1. Additionally, some compounds also showed activity against HIV‐2 (EC~50~=5.82 μM).