Evaluation of secondary amide replacements in a series of CCR5 antagonists as a means to increase intrinsic membrane permeability. Part 1: Optimization of gem-disubstituted azacycles
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- 作者：Ré ; my C. Lemoine ; Ann C. Petersen ; Lina Setti ; Jutta Wanner ; Andreas Jekle ; Gabrielle Heilek ; André ; deRosier ; Changhua Ji ; Pamela Berry ; David Rotstein
- 关键词：CCR5 ; Azacycles ; Intrinsic permeability
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2010
- 出版时间：15 January 2010
- 年：2010
- 卷：20
- 期：2
- 页码：704-708
- 全文大小：642 K
文摘
Replacement of a secondary amide with an N-acyl or N-sulfonyl gem-disubstituted azacyle in a series of CCR5 antagonists led to the identification of compounds with excellent in vitro HIV antiviral activity and increased intrinsic membrane permeability.