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

Structure-activity relationships were performed on a new series of thiazole derivatives which selectively inactivate monoamine oxidase-B (MAO-B), puri fied from mitochondrial beef liver. All of the synthesized and tested compo unds showed non-competitive inhibition, suggesting the formation of a stabl e adduct between the tertiary amine function, linked to the thiazolyl deriv atives 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 at om and the conformational flexibility of the inhibitors.