Benzoxazole piperidines as selective and potent somatostatin receptor subtype 5 antagonists.
Basic Information
ID: ALA1154321
Journal: Bioorg Med Chem Lett
Title: Benzoxazole piperidines as selective and potent somatostatin receptor subtype 5 antagonists.
Authors: Martin RE, Mohr P, Maerki HP, Guba W, Kuratli C, Gavelle O, Binggeli A, Bendels S, Alvarez-Sánchez R, Alker A, Polonchuk L, Christ AD.
Abstract: SAR studies of a recently described SST5R selective benzoxazole piperidine lead series are described with particular focus on the substitution pattern on the benzyl and benzoxazole side-chains. Introduction of a second meta substituent at the benzyl unit significantly lowers residual hH1 activity and insertion of substituents onto the benzoxazole periphery entirely removes remaining h5-HT2B activity. Compounds with single digit nM activity, functional antagonism and favorable physicochemical properties endowed with a good pharmacokinetic profile in rats are described which should become valuable tools for exploring the pharmacological role of the SST5 receptor in vivo.
CiteXplore: 19786348
DOI: 10.1016/j.bmcl.2009.09.024
Patent ID: ┄