Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1373776 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
Abstract
The discovery, synthesis, and preliminary structure–activity relationship (SAR) of a novel class of vasopressin V3 (V1b) receptor antagonists is described. Compound 1, identified by high throughput screening of a diverse, three million-member compound collection, prepared using ECLiPS™ technology, had good activity in a V3 binding assay (IC50 = 0.20 μM), but less than desirable physicochemical properties. Optimization of compound 1 yielded potent analogs 19 (IC50 = 0.31 μM) and 24 (IC50 = 0.12 μM) with improved drug-like characteristics.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Jeffrey J. Letourneau, Christopher M. Riviello, Hong Li, Andrew G. Cole, Koc-Kan Ho, Heather A. Zanetakos, Hema Desai, Jiuqiao Zhao, Douglas S. Auld, Susan E. Napier, Fiona J. Thomson, Katharine A. Goan, J. Richard Morphy, Michael H.J. Ohlmeyer,