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Bioorg Med Chem Lett. 2011 Jun 15;21(12):3603-7. doi: 10.1016/j.bmcl.2011.04.104. Epub 2011 May 1.

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

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  • 1Department of Pharmacology, MSD, Newhouse, Motherwell, United Kingdom.

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 focus on improvement of physicochemical properties, yielding the selective V(1B) antagonist 9f (K(i) 190 nM), with improved druglike characteristics.

Copyright © 2011 Elsevier Ltd. All rights reserved.

PMID:
21601454
[PubMed - indexed for MEDLINE]
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