Identification and characterization of amino-piperidinequinolones and quinazolinones as MCHr1 antagonists

…, V Kadambi, C Doherty, B Dayton, S Brodjian…

Index: Blackburn, Christopher; LaMarche, Matthew J.; Brown, James; Che, Jennifer Lee; Cullis, Courtney A.; Lai, Sujen; Maguire, Martin; Marsilje, Thomas; Geddes, Bradley; Govek, Elizabeth; Kadambi, Vivek; Doherty, Colleen; Dayton, Brian; Brodjian, Sevan; Marsh, Kennan C.; Collins, Christine A.; Kym, Philip R. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 10 p. 2621 - 2627

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Citation Number: 25

Abstract

Several potent, functionally active MCHr1 antagonists derived from quinolin-2 (1H)-ones and quinazoline-2 (1H)-ones have been synthesized and evaluated. Pyridylmethyl substitution at the quinolone 1-position results in derivatives with low-nM binding potency and good selectivity with respect to hERG binding.