Spirodiketopiperazine-based CCR5 antagonists: Lead optimization from biologically active metabolite
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- 作者：Rena Nishizawa ; Toshihiko Nishiyama ; Katsuya Hisaichi ; Naoki Matsunaga ; Chiaki Minamoto ; Hiromu Habashita ; Yoshikazu Takaoka ; Masaaki Toda ; Shiro Shibayama ; Hideaki Tada ; et al.
- 关键词：CCR5 ; HIV-1 ; Active metabolite
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2007
- 出版时间：1 February 2007
- 年：2007
- 卷：17
- 期：3
- 页码：727-731
- 全文大小：181 K
文摘
Hydroxylated derivatives were designed and synthesized based on the information of oxidative metabolites. Compounds derived from β-substituted (2R,3R)-2-amino-3-hydroxypropionic acid showed improved inhibitory activities against the binding of MIP-1α to human CCR5, compared with the non-hydroxylated derivatives and the other isomers.