Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1378468 | Bioorganic & Medicinal Chemistry Letters | 2007 | 5 Pages |
Abstract
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.
Graphical abstractKey modification introducing a hydroxyl group on side chain to improve CCR5 antagonistic activity as well as in vitro anti-HIV activity by the application of the metabolite’s information of 1.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Rena Nishizawa, 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,