Federica Vacondio

TL;DR: The results suggest that anandamide-mediated signaling at peripheral CB1 receptors controls the access of pain-related inputs to the CNS, and brain-impenetrant FAAH inhibitors, which strengthen this gating mechanism, might offer a new approach to pain therapy.

TL;DR: Significant potency improvements were observed for the beta-naphthylmethyl derivative 4q and its 3'-carbamoylbiphenyl-3-yl ester 4z, indicating that shape complementarity and hydrogen bonds are crucial to obtain highly potent inhibitors.

TL;DR: The results suggest that an approach balancing inhibitor reactivity with target recognition produces FAAH inhibitors that display significantly improved drug‐likeness.

TL;DR: The agreement between computations and experiments points to this DFT-based approach as a tool for predicting both nitrile reactivity toward cysteines and the toxicity of nitriles as electrophile agents.

TL;DR: A new series of irreversible inhibitors containing a 3-aminopropanamide linked in position 6 to 4-anilinoquinazoline or 4-anolinoquinoline-3-carbonitrile driving portions is described, which proved to be as efficient as their acrylamide analogues in inhibiting EGFR-TK (TK = tyrosine kinase) autophosphorylation in A549 lung cancer cells.