Potent imidazole and triazole CB1 receptor antagonists related to SR141716

Diarylimidazolecarboxamides and diaryltriazolecarboxamides related to SR141716 were synthesized and tested for binding to the human CB(1) receptor. Suitably substituted imidazoles are comparably potent to the clinical candidate, whereas the analogous triazoles are less so due to the absence of an ad...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2004-03, Vol.14 (5), p.1151-1154
Hauptverfasser:	DYCK, Brian, GOODFELLOW, Val S, PHILLIPS, Teresa, GREY, Jonathan, HADDACH, Mustapha, ROWBOTTOM, Martin, NAEVE, Gregory S, BROWN, Brock, SAUNDERS, John
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological and medical sciences Imidazoles - chemistry Imidazoles - metabolism Medical sciences Miscellaneous Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Piperidines - chemistry Piperidines - metabolism Protein Binding Pyrazoles - chemistry Pyrazoles - metabolism Receptor, Cannabinoid, CB1 - antagonists & inhibitors Receptor, Cannabinoid, CB1 - metabolism Triazoles - chemistry Triazoles - metabolism
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Zusammenfassung:	Diarylimidazolecarboxamides and diaryltriazolecarboxamides related to SR141716 were synthesized and tested for binding to the human CB(1) receptor. Suitably substituted imidazoles are comparably potent to the clinical candidate, whereas the analogous triazoles are less so due to the absence of an additional substituent on the azole ring.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2003.12.068