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Discovery of orally available spirodiketopiperazine-based CCR5 antagonists

Using the previously reported novel spirodiketopiperazine scaffold, the design and synthesis of orally available CCR5 antagonists was undertaken. Compounds possessing 3 carboxylic acid function in the appropriate position showed improved oral exposure (AUC) relative to the initial chemical leads wit...

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Veröffentlicht in:Bioorg Med Chem
Hauptverfasser: Nishizawa, Rena, Nishiyama, Toshihiko, Hisaichi, Katsuya, Hirai, Keisuke, Habashita, Hiromu, Takaoka, Yoshikazu, Tada, Hideaki, Sagawa, Kenji, Shibayama, Shiro, Maeda, Kenji, Mitsuya, Hiroaki, Nakai, Hisao, Fukushima, Daikichi, Toda, Masaaki
Format: Artigo
Sprache:Inglês
Veröffentlicht: 2010
Schlagworte:
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC7566811/
https://ncbi.nlm.nih.gov/pubmed/20542438
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmc.2010.05.057
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