Title of article :
Discovery of potent and stable conformationally constrained analogues of the MCH R1 antagonist SB-568849
Author/Authors :
David R. Witty، نويسنده , , John Bateson، نويسنده , , Guillaume J. Hervieu، نويسنده , , Kamal Al-Barazanji، نويسنده , , Phillip Jeffrey، نويسنده , , Dieter Hamprecht، نويسنده , , Andrea Haynes، نويسنده , , Christopher N. Johnson، نويسنده , , Alison I. Muir، نويسنده , , Peter J. O’Hanlon، نويسنده , , Geoffrey Stemp، نويسنده , , Alex J. Stevens، نويسنده , , Kevin Thewlis، نويسنده , , Kim Y. Winborn، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2006
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.
Keywords :
Benzotriazinone , Thienopyrimidinone , Bicyclic heterocycle , MCH , Biphenylcarboxamide , Antagonist , Melanin-concentrating hormone , obesity , stress , Anxiety , Quinazolinone , cyclisation , MCH R1 , feeding
Journal title :
Bioorganic & Medicinal Chemistry Letters
Journal title :
Bioorganic & Medicinal Chemistry Letters
