Discovery of 4-[4-({(3R)-1-butyl-3-[(R)-cyclohexyl(hydroxy)methyl]-2,5-dioxo-1,4,9-triazaspiro[5.5]undec-9-yl}methyl)phenoxy]benzoic acid hydrochloride: A highly potent orally available CCR5 selective antagonist

Based on the original spirodiketopiperazine design framework, further optimization of an orally available CCR5 antagonist was undertaken. Structural hybridization of the hydroxylated analog 4 derived from one of the oxidative metabolites and the new orally available non-hydroxylated benzoic acid ana...

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Bibliografiske detaljer
Udgivet i:Bioorg Med Chem
Main Authors: Nishizawa, Rena, Nishiyama, Toshihiko, Hisaichi, Katsuya, Minamoto, Chiaki, Murota, Masayuki, Takaoka, Yoshikazu, Nakai, Hisao, Tada, Hideaki, Sagawa, Kenji, Shibayama, Shiro, Fukushima, Daikichi, Maeda, Kenji, Mitsuya, Hiroaki
Format: Artigo
Sprog:Inglês
Udgivet: 2011
Fag:
Article
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC7604827/
https://ncbi.nlm.nih.gov/pubmed/21658961
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmc.2011.05.022
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