Piperazine-1-ium derivative 24a stands out as the first permanently charged CB1R antagonist, exhibiting nanomolar affinity and high CB1R/CB2R selectivity with a favorable physicochemical profile consistent with peripheral restriction and limited blood-brain barrier penetration.
J. Azuaje, Rubén Prieto-Díaz, Claudia Gioé-Gallo et al.· ACS Omega· 0 citations
As dual modulators of Cannabinoid subtype 2 receptor (CB2R) and fatty acid amide hydrolase (FAAH)an arising therapeutic strategy against diseases based on neuroinflammationwe developed a new series of N-adamantyl-benzamides bearing an anthranilic or salicylic scaffold. Derivatives 18, 22, and 25 emerged as an inter...
Giovanni Graziano, Francesco Mastropasqua, A. Fanizzi et al.· Journal of Medicinal Chemist...· 0 citations
This review summarizes recent advances in chemical protein degradation strategies for neurodegenerative disorders and highlights potential future perspectives of multifunctional PROTACs for therapeutic development.
Pasquale Degennaro, Imane Ghafir El Idrissi, Rosa Purgatorio et al.· Pharmaceuticals· 0 citations
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