Parkinson’s disease (PD) is a neurodegenerative disorder mainly characterized by a progressive neurodegeneration
of the dopaminergic neurons. The available pharmacological therapy for PD aims to stop the progress of symptoms,
reduce disability, slowing the neurodegenerative process and/or preventing long-term complications along the therapy.
The main strategic developments that have led to progress in the medical management of PD have focused on improvements
in dopaminergic therapies. Despite all the recent research, there are only a few classes of drugs approved for the
treatment of motor related symptoms of PD which primarily act on the dopaminergic neurons system: L-dopa, dopamine
agonists, monoamine oxidase-B (MAO-B) and catechol-O-methyl transferase (COMT) inhibitors. Anticholinergic drugs
and glutamate antagonists are also available but are not commonly used in routine practice. As no effective therapeutic
strategy has yet been attended, other solutions must be investigated. Privileged structures, such as indoles, arylpiperazines,
biphenyls and benzopyranes are currently ascribed as helpful approaches. Different families of nitrogen and oxygen heterocycles,
such as pyrazoles, hydrazinylthiazoles, xanthones, coumarins or chromones have also been extensively used as
scaffolds in medicinal chemistry programs for searching novel MAO-B inhibitors. Nitrogen derivatives play a key role in
this subject with several studies pointing out hydrazines, thiazoles or indoles as important scaffolds for the development
of novel MAO-B inhibitors. This review comprises an overview of the state of the art on the actual pharmacological therapy
for PD followed by a specific focus on the discovery and development of nitrogen-based heterocyclic compounds
analogues as promising MAO-B inhibitors.