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Identification and characterization of amino-piperidinequinolones and quinazolinones as MCHr1 antagonists
Christopher Blackburn1, Matthew J LaMarche, James Brown
1Millennium Pharmaceuticals, Inc., 40 Landsdowne St. Cambridge, MA 02139, USA. chris.blackburn@mpi.com
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.
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