Published in
Elsevier, Bioorganic and Medicinal Chemistry Letters, 18(19), p. 5351-5354
DOI: 10.1016/j.bmcl.2009.07.130
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Bioisosteric replacement of the hydrazide pharmacophore of the cannabinoid-1 receptor antagonist SR141716A. Part I: Potent, orally-active 1,4-disubstituted imidazoles
Journal article published in 2009 by
Robert L. Dow,
John R. Hadcock,
Dennis O. Scott,
Steven R. Schneider,
Ernest S. Paight,
Philip A. Iredale,
Philip A. Carpino,
David A. Griffith 
,
Marlys Hammond,
Paul Dasilva-Jardine
,
Marlys Hammond,
Paul Dasilva-Jardine
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Abstract
A new series of CB(1) receptor antagonists incorporating an imidazole-based isosteric replacement for the hydrazide moiety of rimonabant (SR141716) is disclosed. Members of this imidazole series possess potent/selective binding to the rCB(1) receptor and exhibit potent hCB(1) functional activity. Isopropyl analog 9a demonstrated activity in the tetrad assay and was orally-active in a food intake model.