2. Academic Validation
  3. Discovery of potent and stable conformationally constrained analogues of the MCH R1 antagonist SB-568849

Discovery of potent and stable conformationally constrained analogues of the MCH R1 antagonist SB-568849

  • Bioorg Med Chem Lett. 2006 Sep 15;16(18):4872-8. doi: 10.1016/j.bmcl.2006.06.061.
David R Witty 1,  John Bateson,  Guillaume J Hervieu,  Kamal Al-Barazanji,  Phillip Jeffrey,  Dieter Hamprecht,  Andrea Haynes,  Christopher N Johnson,  Alison I Muir,  Peter J O'Hanlon,  Geoffrey Stemp,  Alex J Stevens,  Kevin Thewlis,  Kim Y Winborn
Affiliations

Affiliation

  • 1 GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. david.witty@gsk.com
PMID: 16839763 DOI: 10.1016/j.bmcl.2006.06.061
Abstract

A strategy of systematically targeting more rigid analogues of the known MCH R1 receptor antagonist, SB-568849, serendipitously uncovered a binding mode accessible to N-aryl-phthalimide ligands. Optimisation to improve the stability of this compound class led to the discovery of novel N-aryl-quinazolinones, benzotriazinones and thienopyrimidinones as selective ligands with good affinity for human melanin-concentrating hormone receptor 1.

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