Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10594372 | Bioorganic & Medicinal Chemistry Letters | 2012 | 7 Pages |
Abstract
Design, synthesis and SAR analysis of the 5-chloro-4-(4-methoxyphenoxy)-2-(p-toly)pyridazin-3(2H)-one hit, identified through high-through-put screening (HTS) of the Molecular Libraries-Small Molecule Repository, led to the discovery of novel small molecule antagonists of NPBWR1 (GPR7). The lead molecule 5-chloro-2-(3,5-dimethylphenyl)-4-(4-methoxyphenoxy)pyridazin-3(2H)-one 1z (CYM50557) display submicromolar antagonist activity at the target receptor and high selectivity against a panel of therapeutically relevant off-targets. 1z may provide a pharmacological tool to probe the molecular basis of the in vivo physiological function and therapeutic utility of the target receptor in diverse disease areas including inflammatory pain and eating disorders.
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Mariangela Urbano, Miguel Guerrero, Jian Zhao, Subash Velaparthi, S. Adrian Saldanha, Peter Chase, Zhiwei Wang, Olivier Civelli, Peter Hodder, Marie-Therese Schaeffer, Steven Brown, Hugh Rosen, Edward Roberts,