1-Amido-1-phenyl-3-piperidinylbutanes — CCR5 antagonists for the treatment of HIV. Part 1
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- 作者：Christopher G. Barber ; David C. Blakemore ; Jean-Yves Chiva ; Rachel L. Eastwood ; Donald S. Middleton ; Kerry A. Paradowski
- 关键词：HIV ; CCR5 ; Antiviral ; Antagonist
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2009
- 出版时间：15 February 2009
- 年：2009
- 卷：19
- 期：4
- 页码：1075-1079
- 全文大小：953 K
文摘
The development of a new class of CCR5 antagonist replacing the tropane core of maraviroc by piperidine with a branched N-substituent is described. Compound 15h shows good whole cell antiviral activity together with microsomal stability and only weak activity at the hERG ion channel.