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
Mucopolysaccharidosis Type I (MPS I) is a rare autosomal recessive lysosomal storage disorder caused by mutations in α‐ʟ‐iduronidase (IDUA) enzyme, a glycosylated hydrolase responsible for glycosaminoglycan (GAG) degradation. Pathogenic variants are associated with a broad clinical spectrum, from severe Hurler syndrome...
M. Papadopoulos, G. Bonapace, L. Taglietti et al.· Journal of Cellular and Mole...· 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
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