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

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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.

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          Author and article information

          Journal
          Bioorg. Med. Chem. Lett.
          Bioorganic & medicinal chemistry letters
          Elsevier BV
          0960-894X
          0960-894X
          May 15 2006
          : 16
          : 10
          Affiliations
          [1 ] Millennium Pharmaceuticals, Inc., 40 Landsdowne St. Cambridge, MA 02139, USA. chris.blackburn@mpi.com
          Article
          S0960-894X(06)00222-8
          10.1016/j.bmcl.2006.02.044
          16524729
          13979577-7552-4539-a98f-c8afe5ff2cc5
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