Evaluation of amide replacements in CCR5 antagonists as a means to increase intrinsic permeability. Part 2: SAR optimization and pharmacokinetic profile of a homologous azacyle series
详细信息 查看全文
- 作者：Jutta Wanner ; Lijing Chen ; Ré ; my C. Lemoine ; Rama Kondru ; Andreas Jekle ; Gabrielle Heilek ; André ; deRosier ; Changhua Ji ; Pamela W. Berry ; David M. Rotstein
- 关键词：CCR5 antagonist ; HIV entry inhibition ; Permeability
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2010
- 出版时间：15 November 2010
- 年：2010
- 卷：20
- 期：22
- 页码：6802-6807
- 全文大小：927 K
文摘
Replacement of a secondary amide with a piperidine or azetidine moiety in a series of CCR5 antagonists led to the discovery of compounds with increased intrinsic permeability. This effort led to the identification of a potent CCR5 antagonist which exhibited an improved in vivo pharmacokinetic profile.