Discovery of MK-7725, A Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity
文摘
Extensive structure鈥揳ctivity relationship studies of a series derived from atropisomer 1, a previously described chiral benzodiazepine sulfonamide series, led to a potent, brain penetrant and selective compound with excellent preclinical pharmacokinetic across species. We also describe the utilization of a high throughput mouse pharmacodynamic assay which allowed for expedient assessment of pharmacokinetic and brain distribution.
Keywords:
Bombesin receptor subtype-3; BRS-3; agonist; obesity; benzodiazepine sulfonamide; atropisomer; MK-7725