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Identification and optimisation of novel sulfonamide, selective vasopressin V1B receptor antagonists

By James Baker, Matilda Bingham, Ruth Blackburn-Munro, Jiaqiang Cai, Mark Craighead, Robert Gilfillan, Kate Goan, David Jaap, Rachel Milne, J. Richard Morphy, Susan Napier, Jeremy Presland, Gayle Spinks and Fiona Thomson


The synthesis and preliminary structure–activity relationships (SAR) of a novel class of vasopressin V1B receptor antagonists are described. Hit compound 5, identified via high throughput screening of the corporate collection, showed good activity in a V1B binding assay (Ki 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 focus on improvement of physicochemical properties, yielding the selective V1B antagonist 9f (Ki 190 nM), with improved druglike characteristics

Publisher: Elsevier
Year: 2011
OAI identifier:
Provided by: Enlighten
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