2. Academic Validation
  3. Discovery of MK-7725, A Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity

Discovery of MK-7725, A Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity

  • ACS Med Chem Lett. 2012 Jan 21;3(3):252-6. doi: 10.1021/ml200304j.
Harry R Chobanian 1,  Yan Guo 1,  Ping Liu 1,  Marc Chioda 1,  Thomas J Lanza Jr 1,  Linda Chang 1,  Theresa M Kelly 1,  Yanqing Kan 1,  Oksana Palyha 1,  Xiao-Ming Guan 1,  Donald J Marsh 1,  Joseph M Metzger 1,  Judith N Gorski 1,  Kate Raustad 1,  Sheng-Ping Wang 1,  Alison M Strack 1,  Randy Miller 1,  Jianmei Pang 1,  Maria Madeira 1,  Kathy Lyons 1,  Jasminka Dragovic 1,  Marc L Reitman 1,  Ravi P Nargund 1,  Linus S Lin 1
Affiliations

Affiliation

  • 1 Departments of Medicinal Chemistry, Metabolic Disorders, Pharmacology, and Drug Metabolism, Merck Research Laboratories , Rahway, New Jersey 07065, United States.
PMID: 24900461 DOI: 10.1021/ml200304j
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.

Keywords

BRS-3; Bombesin receptor subtype-3; MK-7725; agonist; atropisomer; benzodiazepine sulfonamide; obesity.

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