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Start Over Author "Jag Paul Heer" Journal bioorganicmedicinal chemistry letters
1 results on '"Jag Paul Heer"'

1. Discovery and optimisation of a potent and selective tertiary sulfonamide oxytocin antagonist

Author

Andrew T. Doran, Nick Barton, Benjamin R. Bellenie, Cristian Salvagno, Amanda Emmons, and Jag Paul Heer

Subjects
Models, Molecular, Sulfonamides, Chemistry, Drug discovery, In silico, Organic Chemistry, Clinical Biochemistry, Pharmaceutical Science, Administration, Oral, Pharmacology, Oxytocin, Biochemistry, Oxytocin receptor, Oxytocin Antagonist, Drug Discovery, medicine, Molecular Medicine, Pharmacophore, Molecular Biology, hormones, hormone substitutes, and hormone antagonists, medicine.drug, Vasopressin receptor
Abstract

The optimisation of a tertiary sulfonamide high-throughput screening hit is described. A combination of high-throughput chemistry, pharmacophore analysis and in silico PK profiling resulted in the discovery of potent sulfonamide oxytocin receptor antagonists with oral exposure and good selectivity over vasopressin receptors.

Published
2008

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