Abstract
Catechol-O-methyltransferase (COMT) is a magnesium-dependent enzyme responsible for the catalytic O-methylation reaction of endogenous catecholamines and neurotransmitters. It is also involved in the metabolic process of various hormones and drugs incorporating catecholic structures. COMT has become an attractive biological target in the central nervous system (CNS) disorders associated with dopamine depletion, such as Parkinson’s disease (PD), schizophrenia, and depression. In this chapter, we will provide a thorough description of COMT structural features and its physiopathological roles. Then, we will discuss the different generations of compounds proposed as COMT inhibitors from a medicinal chemistry perspective, including a structure-activity relationship analysis for the best-performing classes of analogues. In addition, updated information about the clinical benefits of the most relevant inhibitors will be highlighted.
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