1. The characterization of a novel V1b antagonist lead series
- Author
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Andrew Green, Chris A. Smethurst, Steve P. Watson, George Burton, Mark J. Schulz, Roberto Arban, Jennifer A. Borthwick, Simon Gaines, and Alberto Buson
- Subjects
Receptors, Vasopressin ,Stereochemistry ,Clinical Biochemistry ,Pharmaceutical Science ,Biochemistry ,Structure-Activity Relationship ,chemistry.chemical_compound ,Drug Discovery ,Animals ,Structure–activity relationship ,Receptor ,Thiazole ,Molecular Biology ,Arginine vasopressin receptor 1B ,Sulfonamides ,Chemistry ,Organic Chemistry ,Antagonist ,Antidiuretic Hormone Receptor Antagonists ,Oxytocin receptor ,High-Throughput Screening Assays ,Rats ,Thiazoles ,Receptors, Oxytocin ,Molecular Medicine ,Selectivity - Abstract
The SAR around a V1b antagonist HTS hit 3 was explored to produce a series of thiazole sulfonamides as a lead series with selectivity over the related V1 and oxytocin receptors.
- Published
- 2011
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