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Discovery of potent and stable conformationally constrained analogues of the MCH R1 antagonist SB-568849 |
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| Authors: | Witty David R Bateson John Hervieu Guillaume J Al-Barazanji Kamal Jeffrey Phillip Hamprecht Dieter Haynes Andrea Johnson Christopher N Muir Alison I O'Hanlon Peter J Stemp Geoffrey Stevens Alex J Thewlis Kevin Winborn Kim Y |
| Affiliation: | GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. david.witty@gsk.com |
| 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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