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2005
Quinoline derivatives
R 0410
Synthesis and Evaluation of 2-Amino-8-alkoxy Quinolines as MCHr1 AntagoPart 2. — To improve the MCHr1 Binding affinity as well as functional potency,
03- 139 nists.
the effect of heteroatoms in the tether at the 8-position of quinoline—based, nontraditional G-protein—coupled receptor ligands is examined. Reductive amination of quinoline derivative (IV) with aliphatic and heterocyclic amines yields potent MCHr1 antagonists. Compounds (VIc), (VId), and (VIe) display single digit nanomolar antagonism of MCHr1-mediated Ca2+ release. The importance of the basic nitrogen in the tether for achieving better brain/plasma distribution is demonstrated with compound (VIa),
which has a longer half-life and better exposure in the brain and plasma compared to
the potent antagonist (VIc). — (VASUDEVAN*, A.; et al.; Bioorg. Med. Chem. Lett.
14 (2004) 19, 4879-4882; Metab. Dis. Res., Abbott Lab., Abbott Park,
IL 60064, USA; Eng.) — H. Hoennerscheid
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