2. Academic Validation
  3. SAR of biphenyl carboxamide ligands of the human melanin-concentrating hormone receptor 1 (MCH R1): discovery of antagonist SB-568849

SAR of biphenyl carboxamide ligands of the human melanin-concentrating hormone receptor 1 (MCH R1): discovery of antagonist SB-568849

  • Bioorg Med Chem Lett. 2006 Sep 15;16(18):4865-71. doi: 10.1016/j.bmcl.2006.06.056.
David R Witty 1,  John H Bateson,  Guillaume J Hervieu,  Phillip Jeffrey,  Christopher N Johnson,  Alison I Muir,  Peter J O'Hanlon,  Geoffrey Stemp,  Alex J Stevens,  Kevin M Thewlis,  Shelagh Wilson,  Kim Y Winborn
Affiliations

Affiliation

  • 1 GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. david.witty@gsk.com
PMID: 16839761 DOI: 10.1016/j.bmcl.2006.06.056
Abstract

We report here the discovery of a class of MCH R1 ligands based on a biphenyl carboxamide template. A docked-in model is presented indicating key interactions in the putative binding site of the receptor. Parallel high throughput synthetic techniques were utilised to allow rapid exploration of the structure-activity relationship around this template, leading to compound SB-568849 which possessed good receptor affinity and selectivity. This compound proved to be an antagonist with stability in vivo, an acceptable brain-blood ratio and oral bioavailability.

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