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2005
Receptor binding activity
X 0280
Synthesis and Evaluation of 2-Amino-8-alkoxy Quinolines as MCHr1 AntagoPart 3. — Previously synthesized 2-amino-8-alkoxyquinoline MCHr1 antago03- 220 nists.
nists possessing acyclic amide-containing side-chains reveal exceptional binding and
functional potency, but negligible CNS penetration. On the other hand, analogues possessing acyclic benzylamine-containing side-chains display improved CNS exposure,
but suffer in functional potency. Constraining the acyclic side-chain by cyclization of
the benzylamine side-chains combines the best features in terms of potency and CNS
penetration among this class of antagonists. Especially compound (I), displaying
sub-nanomolar MCHr1 binding affinity, possesses good functional potency, and excellent CNS exposure. — (SOUERS*, A. J.; et al.; Bioorg. Med. Chem. Lett. 14 (2004)
19, 4883-4886; Metab. Dis. Res., Abbott Lab., Abbott Park, IL 60064, USA; Eng.)
— H. Hoennerscheid
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