Discovery of cyclopentane- and cyclohexane-trans-1,3-diamines as potent melanin-concentrating hormone receptor 1 antagonists

  • Bioorg Med Chem Lett. 2007 Aug 1;17(15):4232-41. doi: 10.1016/j.bmcl.2007.05.034.
Fabrizio Giordanetto  1 ,  Olle Karlsson ,  Jan Lindberg ,  Lars-Olof Larsson ,  Anna Linusson ,  Emma Evertsson ,  David G A Morgan ,  Tord Inghardt
Affiliations
  • 1. Lead Generation, Computational Chemistry, AstraZeneca R&D Mölndal, SE-431 83 Mölndal, Sweden. [email protected]
PMID: 17532215 DOI: 10.1016/j.bmcl.2007.05.034
Abstract

We herein report the optimization of cyclopentane- and cyclohexane-1,3-diamine derivatives as novel and potent MCH-R1 antagonists. Structural modifications of the 2-amino-quinoline and thiophene moieties found in the initial lead compound served to improve its metabolic stability profile and MCH-R1 affinity, and revealed unprecedented SAR when compared to Other 2-amino-quinoline-containing MCH-R1 antagonists.

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