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. 2007 Feb 1;17(3):727-31.
doi: 10.1016/j.bmcl.2006.10.084. Epub 2006 Nov 1.

Spirodiketopiperazine-based CCR5 antagonists: Lead optimization from biologically active metabolite

Rena Nishizawa  1 , Toshihiko Nishiyama, Katsuya Hisaichi, Naoki Matsunaga, Chiaki Minamoto, Hiromu Habashita, Yoshikazu Takaoka, Masaaki Toda, Shiro Shibayama, Hideaki Tada, Kenji Sagawa, Daikichi Fukushima, Kenji Maeda, Hiroaki Mitsuya
Affiliations

Spirodiketopiperazine-based CCR5 antagonists: Lead optimization from biologically active metabolite

Rena Nishizawa et al. Bioorg Med Chem Lett. .

Abstract

Hydroxylated derivatives were designed and synthesized based on the information of oxidative metabolites. Compounds derived from beta-substituted (2R,3R)-2-amino-3-hydroxypropionic acid showed improved inhibitory activities against the binding of MIP-1alpha to human CCR5, compared with the non-hydroxylated derivatives and the other isomers.

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