504434-07-5Relevant academic research and scientific papers
Simple, potent, and selective pyrrole inhibitors of monoamine oxidase types A and B
Silvestri, Romano,La Regina, Giuseppe,De Martino, Gabriella,Artico, Marino,Befani, Olivia,Palumbo, Marianna,Agostinelli, Enzo,Turini, Paola
, p. 917 - 920 (2007/10/03)
N-Benzyl- and N-propargyl-1H-pyrrole-2-carboxyamides and some related methylenamines were synthesized and tested for their monoamine oxidase types A and B inhibitory activity. 2-(N-Methyl-N-propargylaminomethyl)-1H-pyrrole (24) was the most potent MAO-A inhibitor of the series [Ki(MAO-A) = 0.0054 μM], but it was not selective. Inhibitors N-4-fluorobenzyl-1H-pyrrole-2-carboxamide (12) and N-cyclohexylmethyl-1H-pyrrole-2-carboxamide (25) showed the highest MAO-A selectivity indexes (SI) corresponding to 2025 and > 2500, respectively, while 2-(N-methyl-N-benzylaminomethyl)-1H-pyrrole (21) was the most selective MAO-B inhibitor, having an SI of 0.0057.
