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Bioorg Med Chem Lett. 2007 Jul 15;17(14):3978-82. Epub 2007 Apr 29.

Discovery of pyrazine carboxamide CB1 antagonists: the introduction of a hydroxyl group improves the pharmaceutical properties and in vivo efficacy of the series.

Author information

1
Pharmaceutical Research Institute, Bristol Myers Squibb Co., PO Box 5400 Princeton, NJ 08543, USA. Bruce.Ellsworth@bms.com

Abstract

Structure-activity relationships for a series of pyrazine carboxamide CB1 antagonists are reported. Pharmaceutical properties of the series are improved via inclusion of hydroxyl-containing sidechains. This structural modification sufficiently improved ADME properties of an orally inactive series such that food intake reduction was achieved in rat feeding models. Compound 35 elicits a 46% reduction in food intake in ad libidum fed rats 4-h post-dose.

PMID:
17513109
DOI:
10.1016/j.bmcl.2007.04.087
[Indexed for MEDLINE]

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