394249-01-5Relevant academic research and scientific papers
Discovery of potent and stable conformationally constrained analogues of the MCH R1 antagonist SB-568849
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.
, p. 4872 - 4878 (2007/10/03)
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.
