Identification and optimisation of novel sulfonamide, selective vasopressin V₁B receptor antagonists
2011
Baker, James | Bingham, Matilda | Blackburn-Munro, Ruth | Cai, Jiaqiang | Craighead, Mark | Gilfillan, Robert | Goan, Kate | Jaap, David | Milne, Rachel | Richard Morphy, J. | Napier, Susan | Presland, Jeremy | Spinks, Gayle | Thomson, Fiona
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 63nM) 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 190nM), with improved druglike characteristics.
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