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

Abstract Several potent, functionally active MCHr1 antagonists derived from quinolin-2(1 H )-ones and quinazoline-2(1 H )-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.