Antonella Brizzi

TL;DR: A new synthetic route to SC144 is reported and the synthesis of several of its analogues in order to understand required features for activity and modify of the heteroacyl moiety had a dramatic effect on potency.

TL;DR: The new 1-phenyl-5-(1 H-pyrrol-1-yl)pyrazole-3-carboxamides were compared with the reference compounds AM251 and SR144528 for cannabinoid hCB 1 and hCB 2 receptor affinity and a H-bonding interaction was proposed to account for the high affinity for receptors' inactive state and the inverse agonist activity.

TL;DR: This study planned the synthesis of a series of compounds which retained both a rigid structure, like that of plant cannabinoids, and a flexible portion similar to that of anandamide, and showed that some of the newly developed compounds have high affinity and specificity for cannabinoid CB1 and CB2 receptors.

TL;DR: The general loss of potency displayed by the compounds toward clinically relevant mutant strains was deeply studied through a molecular modeling approach, leading to the evidence that the dynamic of the entrance in the non-nucleoside binding pocket could represent the basis of the inhibitory activity of the molecules.

TL;DR: AV1 represents an interesting tool that interacts with G-protein-coupled receptor 40, and was able to enhance insulin secretion dose dependently, behaving as a conceivable agonist of G- protein-couple receptor 40.