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Spirodiketopiperazine-based CCR5 antagonists: Lead optimization from biologically active metabolite |
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| Authors: | Nishizawa Rena Nishiyama Toshihiko Hisaichi Katsuya Matsunaga Naoki Minamoto Chiaki Habashita Hiromu Takaoka Yoshikazu Toda Masaaki Shibayama Shiro Tada Hideaki Sagawa Kenji Fukushima Daikichi Maeda Kenji Mitsuya Hiroaki |
| Affiliation: | Medicinal Chemistry Research Laboratories, Ono Pharmaceutical Co., Ltd, Osaka 618-8585, Japan. r.nishizawa@ono.co.jp |
| 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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