The replacement of amide and alkene groups in a biological setting with the 1,2,3-triazole group led to the discovery of compounds with a unique vanilloid/cannabinoid mixed profile. For example, the natural amides (see picture, above) and their triazole mimics (below) exhibit similar agonistic (X = H) or antagonistic (X = I) activity towards the TRPV1 receptor; however, only the triazole derivatives also show cannabinomimetic activity.

The 1,2,3-triazole ring as a peptido- and olefinomimetic element: discovery of click vanilloids and cannabinoids

De Petrocellis L;Di Marzo V
2007

Abstract

The replacement of amide and alkene groups in a biological setting with the 1,2,3-triazole group led to the discovery of compounds with a unique vanilloid/cannabinoid mixed profile. For example, the natural amides (see picture, above) and their triazole mimics (below) exhibit similar agonistic (X = H) or antagonistic (X = I) activity towards the TRPV1 receptor; however, only the triazole derivatives also show cannabinomimetic activity.
2007
Istituto di Chimica Biomolecolare - ICB - Sede Pozzuoli
Istituto di Scienze Applicate e Sistemi Intelligenti "Eduardo Caianiello" - ISASI
cannabinoids
cycloaddition
drug design
triazoles
vanilloids
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/20.500.14243/144791
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