Potent imidazole and triazole CB1 receptor antagonists related to SR141716.

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Dyck B, Goodfellow VS, Phillips T, Grey J, Haddach M, Rowbottom M, Naeve GS, Brown B, Saunders J

Potent imidazole and triazole CB1 receptor antagonists related to SR141716.

Bioorg Med Chem Lett. 2004 Mar 8;14(5):1151-4.

PubMed ID

14980654 [ View in PubMed

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Abstract

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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Rimonabant	Cannabinoid receptor 1	Ki (nM)	12	N/A	N/A	Details