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Your search keyword '"Zhao, Jiuqiao"' showing total 1 results
Start Over Author "Zhao, Jiuqiao" Topic antagonist
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1. Identification and optimization of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V3 (V1b) receptor antagonists

Author

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., and Webb, Maria L.

Subjects
*ORGANIC synthesis, *VASOPRESSIN, *STRUCTURE-activity relationship in pharmacology, *HORMONE receptors, *HORMONE antagonists, *HYPOTHALAMIC-pituitary-adrenal axis
Abstract

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 =0.20μM), but less than desirable physicochemical properties. Optimization of compound 1 yielded potent analogs 19 (IC50 =0.31μM) and 24 (IC50 =0.12μM) with improved drug-like characteristics. [ABSTRACT FROM AUTHOR]

Published
2010
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