Heterocyclic Chemistry in Drug Discovery

Dear Colleagues,

New advances in synthetic methodologies that allow access to a wide variety of functionalized heterocycles are of critical importance to any scientist involved in medicinal and process chemistry aspects of drug discovery research and development. Furthermore, the recent progress of both transition metal catalysts and organocatalysts could enable easy access to available, scalable, and eco-friendly methodologies.

The first cases in the recent pandemic caused by SARS-CoV-2 were reported in Wuhan, China, and this virus was subsequently reported in 218 countries and territories. As of 2 November 2020, the World Health Organization reported 46,403,652 confirmed cases and a death toll of 1,198,569. Despite the efforts by researchers in the pharmaceutical industry and research centers of universities, no suitable medications are currently available against SARS-CoV-2. The emergence of epidemics due to two coronaviruses, severe acute respiratory syndrome (SARS) and Middle East respiratory syndrome (MARS), which are associated with severe mortality rates, prompted the development of a collection of drug candidates that may act against SARS-CoV-2 and are characterized by a range of heterocyclic nuclei: isatin and indoles; pyridine, quinolines, and isoquinolines; purine and pyrimidines; thiazoles; pyrazoles; and triazoles.

In addition to SARS-CoV-2, drugs and drug candidates for treating other life-threatening diseases often contain the N-containing heterocycles of different ring sizes, bearing different heteroatoms like oxygen and sulfur. New insights into the synthesis and synthetic methodologies of the heterocyclic motif would help to accelerate the drug development process. In the past decade, 4732 published reviews on heterocycles and heterocyclic chemistry have emerged from various academic disciplines, including chemistry, pharmacy, and materials. In particular, new robust synthetic methodologies relying on the use of practical and useful intermediates (e.g., radicals, cations, anions, carbenes, nitrenes, and benzynes) have been devised and successfully applied to the synthesis of heterocycles and fused derivatives.

This Special Issue of Molecules will comprise original research articles and reviews in the area of heterocycle chemistry considering synthesis and synthetic intermediates affording easy access to heterocycles and fused heterocycles that help to accelerate the drug discovery.

Prof. Dr. Mitsuhiro Yoshimatsu
Guest Editor

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• heterocycles
• synthetic methodologies
• functionalizations
• drug discovery
• N-containing heterocycles
• radicals
• cations
• anions
• carbenes
• nitrenes
• benzynes