Selective Inhibitory Activity against MAO and Molecular Modeling Studies of 2-Thiazolylhydrazone Derivatives
Journal of Medicinal Chemistry2007Vol. 50(4), pp. 707–712
Citations Over TimeTop 10% of 2007 papers
Franco Chimenti, Elias Maccioni, Daniela Secci, Adriana Bolasco, Paola Chimenti, Arianna Granese, Olivia Befani, Paola Turini, Stefano Alcaro, Francesco Ortuso, Maria Cristina Cardia, Simona Distinto
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 pKi 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.
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