Bioorganic & Medicinal Chemistry Letters 2006-05-15

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

Christopher Blackburn, Matthew J LaMarche, James Brown, Jennifer Lee Che, Courtney A Cullis, Sujen Lai, Martin Maguire, Thomas Marsilje, Bradley Geddes, Elizabeth Govek, Vivek Kadambi, Colleen Doherty, Brian Dayton, Sevan Brodjian, Kennan C Marsh, Christine A Collins, Philip R Kym

Index: Bioorg. Med. Chem. Lett. 16(10) , 2621-7, (2006)

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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.