A series of 2-thiazolylhydrazone derivatives have been investigated for the ability to inhibit the activity of the A and B isoforms of monoamine oxidase (MAO) selectively. All of the compounds showed high activity against both the MAO-A and the MAO-B isoforms with pK(i) values ranging between 5.92 and 8.14 for the MAO-A and between 4.69 and 9.09 for the MAO-B isoforms. Both the MAO-A and the MAO-B isoforms, deposited in the Protein Data Bank as model 2BXR and 1GOS, respectively, were considered in a computational study performed with docking techniques on the most active and MAO-B-selective inhibitor, 18.
Selective inhibitory activity against MAO and molecular modeling studies of 2-thiazolylhydrazone derivatives / Chimenti, Franco; Elias, Maccioni; Secci, Daniela; Bolasco, Adriana; Chimenti, Paola; Granese, Arianna; Olivia, Befani; Turini, Paola; Stefano, Alcaro; Francesco, Ortuso; Maria C., Cardia; Simona, Distinto. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - 50:4(2007), pp. 707-712. [10.1021/jm060869d]
Selective inhibitory activity against MAO and molecular modeling studies of 2-thiazolylhydrazone derivatives
CHIMENTI, Franco;SECCI, DANIELA;BOLASCO, Adriana;CHIMENTI, Paola;GRANESE, ARIANNA;TURINI, Paola;
2007
Abstract
A series of 2-thiazolylhydrazone derivatives have been investigated for the ability to inhibit the activity of the A and B isoforms of monoamine oxidase (MAO) selectively. All of the compounds showed high activity against both the MAO-A and the MAO-B isoforms with pK(i) values ranging between 5.92 and 8.14 for the MAO-A and between 4.69 and 9.09 for the MAO-B isoforms. Both the MAO-A and the MAO-B isoforms, deposited in the Protein Data Bank as model 2BXR and 1GOS, respectively, were considered in a computational study performed with docking techniques on the most active and MAO-B-selective inhibitor, 18.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
