Monoamine oxidase B (MAO B) is of clinical importance due to its perceived role in neurodegenerative diseases such as Parkinson’s, making inhibitors of MAO B popular candidates for drug design. A series of coumarin derivatives have been prepared and assayed, revealing that the synthesized inhibitors act through a competitive mode of inhibition. In addition, these inhibitors are potent with Ki values in the nanomolar range. Overall, substitution at the 3- position of the coumarin was found to be important to inhibitor potency and further study of 3-aryl coumarin substitution computationally led to the prediction of 3-(3-aminophenyl)-6-hydroxycoumarin as a lead compound for future study as a more potent MAO B inhibitor.
Kieffer, Ian A., "Synthesis and Evaluation of Substituted Coumarin Derivatives as Inhibitors of Monoamine Oxidase B" (2015). Chemistry Theses. 1.