Inhibition of monoamine oxidase by 8-benzyloxycaffeine analogues

B Strydom, SF Malan, N Castagnoli, JJ Bergh…

Index: Strydom, Belinda; Malan, Sarel F.; Castagnoli Jr., Neal; Bergh, Jacobus J.; Petzer, Jacobus P. Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 3 p. 1018 - 1028

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Citation Number: 70

Abstract

Based on recent reports that several (E)-8-styrylcaffeinyl analogues are potent reversible inhibitors of monoamine oxidase B (MAO-B), a series of 8-benzyloxycaffeinyl analogues were synthesized and evaluated as inhibitors of baboon liver MAO-B and recombinant human MAO-A and-B. The 8-benzyloxycaffeinyl analogues were found to inhibit reversibly both MAO isoforms with enzyme–inhibitor dissociation constants (Ki values) ranging from ...