Heteroatoms can be found in a number of biologically active substances, active pharmaceutical ingredients, and excipients. In particular, many nitrogen heterocycles are considered as privileged scaffolds because more than 85% of all biologically-active chemical entities are endowed with a heterocycle and approximately 60% of FDA-approved drugs contain the nitrogen atom in their structure.

Nitrogen heterocycles have been shown to exhibit a very wide range of biological activities mimicking natural compounds or endogenous metabolites. This topic reflects the crucial role of nitrogen heterocycles in modern drug design and development and their therapeutic potential. Moreover, the presence of heterocycles could provide an improvement of the ADME/Tox properties. A wide chemical diversity can be attained by alternative and green synthetic methodologies to improve Structure-Activity Relationships (SARs).

The aim of this Special Issue is to collate articles providing new insights into nitrogen heterocycles in medicinal chemistry. Original research and review articles are welcome.

Potential topics include but are not limited to the following:

• Characterization of new chemical entities
• Derivatives from natural compounds
• Biomaterials
• Drug design
• In silico investigations
• Biological screening
• Isolation from natural matrices of new nitrogen heterocycles
• Novel approaches in synthesis
• Drug release and targeting
• Toxicity