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Literature DB >> 17118654

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

Rena Nishizawa¹, 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.

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.

Entities: Chemical Gene Species

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Year: 2006 PMID： 17118654 DOI： 10.1016/j.bmcl.2006.10.084

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

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Cited

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