1247950-19-1Relevant articles and documents
Identification and optimization of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)- yl)acetamide vasopressin V3 (V1b) receptor antagonists
Letourneau, Jeffrey J.,Riviello, Christopher M.,Li, Hong,Cole, Andrew G.,Ho, Koc-Kan,Zanetakos, Heather A.,Desai, Hema,Zhao, Jiuqiao,Auld, Douglas S.,Napier, Susan E.,Thomson, Fiona J.,Goan, Katharine A.,Morphy, J. Richard,Ohlmeyer, Michael H.J.,Webb, Maria L.
scheme or table, p. 5394 - 5397 (2010/12/25)
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.
