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J Enzyme Inhib. 1999;14(4):307-21.

Thiazole derivatives as inhibitors of purified bovine liver mitochondrial monoamine oxidase-B: structure-activity relationships and theoretical study.

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Istituto di Scienze Biochimiche e Farmacologiche, University of Catania, Italy.


Structure-activity relationships were performed on a new series of thiazole derivatives which selectively inactivate monoamine oxidase-B (MAO-B), purified from mitochondrial beef liver. All of the synthesized and tested compounds showed non-competitive inhibition, suggesting the formation of a stable adduct between the tertiary amine function, linked to the thiazolyl derivatives and the active site of the enzyme. The mechanism of MAO-B inhibition is discussed in terms of the Ionization Potential of the amine nitrogen atom and the conformational flexibility of the inhibitors.

[Indexed for MEDLINE]

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