期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 19, 期 13, 页码 4028-4042出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2011.05.022
关键词
CCR5; Chemokine; Anti-HIV-1
资金
- Intramural NIH HHS [Z01 BC011109] Funding Source: Medline
Based on the original spirodiketopiperazine design framework, further optimization of an orally available CCR5 antagonist was undertaken. Structural hybridization of the hydroxylated analog 4 derived from one of the oxidative metabolites and the new orally available non-hydroxylated benzoic acid analog 5 resulted in another potent orally available CCR5 antagonist 6a as a clinical candidate. Full details of a structure-activity relationship (SAR) study and ADME properties are presented. (C) 2011 Elsevier Ltd. All rights reserved.
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