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Bioorg Med Chem Lett. 2009 Mar 15;19(6):1564-8. doi: 10.1016/j.bmcl.2009.02.035. Epub 2009 Feb 12.

Identification of novel and orally active spiroindoline NPY Y5 receptor antagonists.

Author information

1
Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba 300-2611, Japan.

Abstract

A series of spiroindoline-3,4'-piperidine derivatives were synthesized and evaluated for their binding affinities and antagonistic activities at Y5 receptors. Potent Y5 antagonists were tested for their oral bioavailabilities and brain penetration in rats. Some of the antagonists showed good oral bioavailability and/or good brain penetration. In particular, compound 6e was orally bioavailable and brain penetrant, and oral administration of 6e inhibited bPP-induced food intake in rats with a minimum effective dose of 10mg/kg.

PMID:
19243937
DOI:
10.1016/j.bmcl.2009.02.035
[Indexed for MEDLINE]

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