Focusing on the importance of the free phenolic hydroxyl moiety, a family of 23 alkylresorcinol-based compounds were developed and evaluated for their cannabinoid receptor binding properties. The non-symmetrical hexylresorcinol derivative 29 turned out to be a CB2-selective competitive antagonist/inverse agonist endowed with good potency. Both the olivetol- and 5-(2-methyloctan-2-yl)resorcinol-based derivatives 23 and 24 exhibited a significant antinociceptive activity. Interestingly, compound 24 proved to be able to activate both cannabinoid and TRPV1 receptors. Even if cannabinoid receptor subtype selectivity remained a goal only partially achieved, results confirm the validity of the alkylresorcinol nucleus as skeleton for the identification of potent cannabinoid receptor modulators.
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Titolo: | Synthetic bioactive olivetol-related amides: The influence of the phenolic group in cannabinoid receptor activity |
Autori: | |
Data di pubblicazione: | 2020 |
Rivista: | |
Handle: | http://hdl.handle.net/20.500.11770/307742 |
Appare nelle tipologie: | 1.1 Articolo in rivista |