New pyrrole inhibitors of monoamine oxidase: synthesis, biological evaluation, and structural determinants of MAO-A and MAO-B selectivity

G La Regina, R Silvestri, M Artico…

文献索引：Silvestri, Romano; La Regina, Giuseppe; De Martino, Gabriella; Artico, Marino; Befani, Olivia; Palumbo, Marianna; Agostinelli, Enzo; Turini, Paola Journal of Medicinal Chemistry, 2003 , vol. 46, # 6 p. 917 - 920

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被引用次数: 83

摘要

A series of new pyrrole derivatives have been synthesized and evaluated for their monoamine oxidase (MAO) A and B inhibitory activity and selectivity. N-Methyl, N-(benzyl), N-(pyrrol-2-ylmethyl) amine (7) and N-(2-benzyl), N-(1-methylpyrrol-2-ylmethyl) amine (18) were the most selective MAO-B (7, SI= 0.0057) and MAO-A (18, SI= 12500) inhibitors, respectively. Docking and molecular dynamics simulations gave structural insights into the ...