Product Details of 100-51-6. Chavarria, D; Fernandes, C; Silva, V; Silva, C; Gil-Martins, E; Soares, P; Silva, T; Silva, R; Remiao, F; Oliveira, PJ; Borges, F in [Chavarria, Daniel; Fernandes, Carlos; Silva, Vera; Silva, Catia; Gil-Martins, Eva; Soares, Pedro; Silva, Tiago; Borges, Fernanda] Univ Porto, Fac Sci, Dept Chem & Biochem, CIQUP, Porto, Portugal; [Chavarria, Daniel; Silva, Tiago; Oliveira, Paulo J.] Univ Coimbra, UC Biotech, CNC Ctr Neurosci & Cell Biol, Biocant Pk, Cantanhede, Portugal; [Silva, Vera; Gil-Martins, Eva; Silva, Renata; Remiao, Fernando] Univ Porto, Fac Pharm, Dept Biol Sci, UCIBIO,REQUIMTE,Lab Toxicol, Porto, Portugal published Design of novel monoamine oxidase-B inhibitors based on piperine scaffold: Structure-activity-toxicity, drug-likeness and efflux transport studies in 2020.0, Cited 58.0. The Name is Benzyl Alcohol. Through research, I have a further understanding and discovery of 100-51-6.
Piperine has been associated with neuroprotective effects and monoamine oxidase (MAO) inhibition, thus being an attractive scaffold to develop new antiparkinsonian agents. Accordingly, we prepared a small library of piperine derivatives and screened the inhibitory activities towards human MAO isoforms (hMAO-A and hMAO-B). Structure-activity relationship (SAR) studies pointed out that the combination of alpha-cyano and benzyl ester groups increased both potency and selectivity towards hMAO-B. Kinetic experiments with compounds 7, 10 and 15 indicated a competitive hMAO-B inhibition mechanism. Compounds 15 and 16, at 10 mu M, caused a small but significant decrease in P-gp efflux activity in Caco-2 cells. Compound 15 stands out as the most potent piperine-based hMAO-B inhibitor (IC50 = 47.4 nM), displaying favourable drug-like properties and a broad safety window. Compound 15 is thus a suitable candidate for lead optimization and the development of multitarget-directed ligands. (C) 2019 Elsevier Masson SAS. All rights reserved.
About Benzyl Alcohol, If you have any questions, you can contact Chavarria, D; Fernandes, C; Silva, V; Silva, C; Gil-Martins, E; Soares, P; Silva, T; Silva, R; Remiao, F; Oliveira, PJ; Borges, F or concate me.. Product Details of 100-51-6
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