Novel hexahydropyrrolo[3,4-c]pyrrole CCR5 antagonists
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- 作者：David M. Rotstein ; Chris R. Melville ; Fern ; o Padilla ; Dick Cournoyer ; Eun K. Lee ; Remy Lemoine ; Ann C. Petersen ; Lina Q. Setti ; Jutta Wanner ; Lijing Chen ; Lubov Filonova ; David G. Loughhead ; Jason Man
- 关键词：CCR5 antagonist ; Chemokine ; Anti-HIV-1 ; Antiviral
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2010
- 出版时间：15 May 2010
- 年：2010
- 卷：20
- 期：10
- 页码：3116-3119
- 全文大小：3016 K
文摘
Starting with a high-throughput screening lead, a novel series of CCR5 antagonists was developed utilizing an information-based approach. Improvement of pharmacokinetic properties for the series was pursued by SAR exploration of the lead template. The synthesis, SAR and biological profiles of the series are described.