Identification and optimisation of novel sulfonamide, selective vasopressin V 1B receptor antagonists

J Baker, M Bingham, R Blackburn-Munro, J Cai…

文献索引：Baker, James; Bingham, Matilda; Blackburn-Munro, Ruth; Cai, Jiaqiang; Craighead, Mark; Gilfillan, Robert; Goan, Kate; Jaap, David; Milne, Rachel; Richard Morphy; Napier, Susan; Presland, Jeremy; Spinks, Gayle; Thomson, Fiona Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 12 p. 3603 - 3607

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被引用次数: 1

摘要

Abstract The synthesis and preliminary structure–activity relationships (SAR) of a novel class of vasopressin V 1B receptor antagonists are described. Hit compound 5, identified via high throughput screening of the corporate collection, showed good activity in a V 1B binding assay (K i 63 nM) but did not possess the lead-like physicochemical properties typically required in a hit compound. A 'deletion approach'on the HTS hit 5 was performed, with the ...