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Bioorg Med Chem. 2011 Jul 1;19(13):4028-42. doi: 10.1016/j.bmc.2011.05.022. Epub 2011 May 20.

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.

Author information

1
Medicinal Chemistry Research Laboratory, Ono Pharmaceutical Co. Ltd, Shimamoto, Mishima, Osaka, Japan. r.nishizawa@ono.co.jp

Abstract

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 analog 5 resulted in another potent orally available CCR5 antagonist 6a as a clinical candidate. Full details of a structure-activity relationship (SAR) study and ADME properties are presented.

PMID:
21658961
DOI:
10.1016/j.bmc.2011.05.022
[Indexed for MEDLINE]
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