Discovery of MK-7725, A Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity
ACS Medicinal Chemistry Letters2012Vol. 3(3), pp. 252–256
Citations Over TimeTop 11% of 2012 papers
Harry R. Chobanian, Yan Guo, Ping Liu, Marc Chioda, Thomas J. Lanza, Linda Chang, Theresa M. Kelly, Yanqing Kan, Oksana Palyha, Xiao-Ming Guan, Donald J. Marsh, Joseph M. Metzger, Judith N. Gorski, Kate A. Raustad, Sheng-Ping Wang, Alison M. Strack, Randy R. Miller, Jianmei Pang, Maria Madeira, Kathy Lyons, Jasminka Dragovic, Marc L. Reitman, Ravi P. Nargund, Linus S. Lin
Abstract
Extensive structure-activity 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.
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