2. Academic Validation
  3. The design and synthesis of potent, selective benzodiazepine sulfonamide bombesin receptor subtype 3 (BRS-3) agonists with an increased barrier of atropisomerization

The design and synthesis of potent, selective benzodiazepine sulfonamide bombesin receptor subtype 3 (BRS-3) agonists with an increased barrier of atropisomerization

  • Bioorg Med Chem. 2012 May 1;20(9):2845-9. doi: 10.1016/j.bmc.2012.03.029.
Harry R Chobanian 1,  Yan Guo,  Ping Liu,  Thomas J Lanza Jr,  Marc Chioda,  Linda Chang,  Theresa M Kelly,  Yanqing Kan,  Oksana Palyha,  Xiao-Ming Guan,  Donald J Marsh,  Joseph M Metzger,  Katie Raustad,  Sheng-Ping Wang,  Alison M Strack,  Judith N Gorski,  Randy Miller,  Jianmei Pang,  Kathy Lyons,  Jasminka Dragovic,  Jian G Ning,  Wes A Schafer,  Christopher J Welch,  Xiaoyi Gong,  Ying-Duo Gao,  Viktor Hornak,  Marc L Reitman,  Ravi P Nargund,  Linus S Lin
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. harry_chobanian@merck.com
PMID: 22494842 DOI: 10.1016/j.bmc.2012.03.029
Abstract

Bombesin Receptor subtype 3 (BRS-3) is an orphan G-protein coupled receptor expressed primarily in the hypothalamus which plays a role in the onset of both diabetes and obesity. We report herein our progress made towards identifying a potent, selective Bombesin Receptor subtype-3 (BRS-3) agonist related to the previously described MK-7725(1) Chobanian et al. (2012) that would prevent atropisomerization through the increase of steric bulk at the C-2 position. This would thereby make clinical development of this class of compounds more cost effective by inhibiting racemization which can occur over long periods of time at room/elevated temperature.

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