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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.
Afiliación
  • Silvestri R; Dipartimento di Studi Farmaceutici, Università degli Studi di Roma La Sapienza, P.le Aldo Moro, 5, I-00185 Roma, Italy. romano.silvestri@uniroma1.it
J Med Chem ; 46(6): 917-20, 2003 Mar 13.
Article en En | MEDLINE | ID: mdl-12620068
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 [K(i)(MAO-A) = 0.0054 microM], 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.
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirroles / Alquinos / Monoaminooxidasa / Inhibidores de la Monoaminooxidasa Límite: Animals Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2003 Tipo del documento: Article País de afiliación: Italia Pais de publicación: Estados Unidos
Buscar en Google
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PubMed Links

Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirroles / Alquinos / Monoaminooxidasa / Inhibidores de la Monoaminooxidasa Límite: Animals Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2003 Tipo del documento: Article País de afiliación: Italia Pais de publicación: Estados Unidos