Chemicals and Drugs Commons^™

Synthesis And Evaluation Of Substituted Coumarin Derivatives As Inhibitors Of Monoamine Oxidase B, Ian A. Kieffer

Chemistry Theses

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 …