Discovery and Lead Optimization of Atropisomer D1 Agonists with Reduced Desensitization.
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DOI: 10.1021/acs.jmedchem.8b01622
Abstract: The discovery of D1 subtype-selective agonists with drug-like properties has been an enduring challenge for the greater part of 40 years. All known D1-selective agonists are catecholamines that bring about receptor desensitization and undergo rapid… read more here.
Keywords: atropisomer; lead optimization; discovery; discovery lead ... See more keywords
Characterization of Stereoselective Metabolism, Inhibitory Effect on Uric Acid Uptake Transporters, and Pharmacokinetics of Lesinurad Atropisomers
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DOI: 10.1124/dmd.118.080549
Abstract: Lesinurad [Zurampic; 2-(5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)], a selective inhibitor of uric acid reabsorption transporters approved for the treatment of gout, is a racemate of two atropisomers. The objective of this investigation was to evaluate the stereoselectivity of metabolism,… read more here.
Keywords: atropisomer; uric acid; metabolism inhibitory; lesinurad atropisomers ... See more keywords