Inhibition of monoamine oxidase B by selected benzimidazole and caffeine analogues

…, MO Ogunrombi, SF Malan, G Terre'Blanche…

Index: van den Berg, Deidre; Zoellner, Kevin R.; Ogunrombi, Modupe O.; Malan, Sarel F.; Terre'Blanche, Gisella; Castagnoli Jr., Neal; Bergh, Jacobus J.; Petzer, Jacobus P. Bioorganic and Medicinal Chemistry, 2007 , vol. 15, # 11 p. 3692 - 3702

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Citation Number: 61

Abstract

We have recently reported that a series of (E)-8-styrylcaffeines and (E)-2- styrylbenzimidazoles are moderate to very potent competitive inhibitors of monoamine oxidase B (MAO-B). The most potent member of the series was found to be (E)-8-(3- chlorostyryl) caffeine (CSC) with an enzyme-inhibitor dissociation constant (Ki value) of 128nM. In the present study, we have prepared additional caffeine and benzimidazole ...