- Identification and characterization of amino-piperidinequinolones and quinazolinones as MCHr1 antagonists.
Identification and characterization of amino-piperidinequinolones and quinazolinones as MCHr1 antagonists.
Bioorganic & medicinal chemistry letters (2006-03-10)
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
PMID16524729
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.
MATERIALS