Design, synthesis and SAR analysis of novel potent and selective small molecule antagonists of NPBWR1 (GPR7)

…, M Guerrero, J Zhao, S Velaparthi, SA Saldanha…

Index: Urbano, Mariangela; Guerrero, Miguel; Zhao, Jian; Velaparthi, Subash; Roberts, Edward; Adrian Saldanha, S.; Chase, Peter; Hodder, Peter; Wang, Zhiwei; Civelli, Olivier; Schaeffer, Marie-Therese; Brown, Steven; Rosen, Hugh Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 23 p. 7135 - 7141,7

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Citation Number: 2

Abstract

Novel small molecule antagonists of NPBWR1 (GPR7) are herein reported. A high- throughput screening (HTS) of the Molecular Libraries-Small Molecule Repository library identified 5-chloro-4-(4-methoxyphenoxy)-2-(p-tolyl) pyridazin-3 (2H)-one as a NPBWR1 hit antagonist with micromolar activity. Design, synthesis and structure–activity relationships study of the HTS-derived hit led to the identification of 5-chloro-2-(3, 5-dimethylphenyl)-4-( ...