Tetrahydroisoquinolines as MCH-R1 antagonists

descriptionPublicationkeyboard_double_arrow_right Article 01 Sep 2006 English Publisher:Elsevier BVJournal:Bioorganic & Medicinal Chemistry Letters, volume 16, pages 4,917-4,921 (issn: 0960-894X,

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Authors: T K, Sasikumar; L, Qiang; W-L, Wu; D A, Burnett; W J, Greenlee; K, O'Neill; B E, Hawes; +2 Authors

doi: 10.1016/j.bmcl.2006.06.055

pmid: 16824753

Tetrahydroisoquinolines as MCH-R1 antagonists

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Abstract

A series of potent and selective inhibitors of h-MCH-R1 has been developed based on the piperidine glycineamide compounds I and II. These structurally more rigid tetrahydroisoquinolines (III and IV) showed better pharmacokinetics. The highly potent compounds 12d and 12g displayed excellent rat pk.

Related Organizations

Schering-Plough
United States

Keywords

Structure-Activity Relationship, Molecular Structure, Tetrahydroisoquinolines, Animals, Humans, Benzimidazoles, Receptors, Somatostatin, Rats

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