Dear Colleagues,

Most of the organic compounds used as therapeutics, as well as intermediates utilized for their synthesis, contain heterocyclic motifs. A heterocycle is a ring with at least one atom that is not carbon. Nitrogen, oxygen, and sulfur are the primary elements seen in common heterocycles and play a critical role in drug discovery. In detail, nitrogen heterocycles contain at least one nitrogen atom in the ring. Based on the size of the ring, there are three, four, five, six, seven and eight-membered rings, as well as fused, bicyclic and macrocyclic heterocycles of nitrogen. Furthermore, these may be described as aromatic, saturated or unsaturated. Depending on the structure and on the type of bonds, such compounds show different acid–base properties and can contain one, two or more nitrogen atoms. Nitrogen-containing scaffolds are among the most significant structural components of therapeutic agents. Furthermore, there are a plethora of natural products which are nitrogen-containing heterocyclic that serve as the basis for many different substances, including alkaloids, vitamins, hormones, dyes, antibiotics, herbicides, or nutraceuticals.  Over the past decades, much attention has been devoted to the development of and pharmacological studies into heteroaromatic organic compounds (such as benzimidazoles, benzothiazoles, indole, oxadiazole, imidazole, isoxazole, pyrazole, triazoles, quinolines and quinazolines) that are currently considered privileged scaffolds for different therapeutic agents. Indeed, they show a wide range of biological activities, representing nearly 60% of all FDA-approved drugs, with more than 880 nitrogen-based heterocyclic drugs approved by the US FDA. For instance, nitrogen-based heterocyclic compounds are widely reported in the literature as anticancer agents and represented 73% of the approved anticancer drugs in 2015. This Special Issue will publish research papers with topics including, but not limited to, the preparation of aromatic and non-aromatic nitrogen-containing heterocycles endowed with any biological action. We also welcome contributions that highlight the importance of the nitrogen-based scaffolds that are widely found in agrochemicals, dyes, cosmetics and functional materials. The aim of the present Special Issue is primarily to present an overview primarily of the state of the art of synthetic methods and recent advances in the synthesis of nitrogen-based heterocycles.

Dr. Valentina Noemi Madia
Dr. Valeria Tudino
Guest Editors

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• nitrogen-based heterocycles
• bioactive compounds
• structure-based drug design
• structure-activity relationship
• in silico studies
• ADMET properties
• microwave-assisted synthesis
• green chemistry
• multicomponent reactions
• phytochemicals