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Identification and optimization of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V3 (V1b) receptor antagonists
- Source :
-
Bioorganic & Medicinal Chemistry Letters . Sep2010, Vol. 20 Issue 18, p5394-5397. 4p. - Publication Year :
- 2010
-
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]
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 20
- Issue :
- 18
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 53333745
- Full Text :
- https://doi.org/10.1016/j.bmcl.2010.07.118