Many nitrogen heterocycles are widely found in natural products, organic materials, agrochemicals, and pharmaceuticals. There are three important areas within heterocyclic chemistry from the perspective of medicinal chemists. Firstly, nature is capable of generating a vast array of complex molecules; to find and evaluate bioactive natural products containing nitrogen heterocycles is critical to the achievement of drug discovery. Secondly, a number of methods to synthesize nitrogen heterocycles are based on the cyclization of acyclic precursors. However, many of these approaches involve the use of expensive/toxic reagents and harsh conditions, hence the continuous need for new and more sustainable synthetic approaches is of particular interest. Lastly, the use of C-H bond functionalization to generate analogues of a sophisticated molecular structure has been identified as an effective strategy; the C-H functionalization of nitrogen heterocycles offers new opportunities in drug discovery. So, the ability to obtain heterocycles with great structural diversity remains an important goal.
More than 75% of drugs approved by the FDA and currently available in the market are nitrogen-containing heterocyclic moieties. In view of this, the goal of this research topic is to highlight recent developments in isolation, construction, and C-H functionalization of nitrogen heterocycles for drug discovery. Research on exploring nitrogen heterocycles from natural resources, such as isolation; structural identification; biological evaluation; and optimization of the extraction process is one of our interests. We also wish to emphasize the importance of novel and efficient synthetic methods and mechanisms for the construction and late-stage modification of nitrogen heterocycles by C-H functionalization.
This Topic welcomes high-quality research including Original Research Articles, Reviews, Mini-Reviews, Perspectives, based on but not limited to the following themes:
• The isolation and structure elucidation of novel nitrogen heterocycles from nature
• Optimization of the extraction process of bioactive nitrogen heterocycles from nature
• Design, synthesis and biological evaluation of nitrogen-containing heterocycles
• Development of new synthetic methods for the construction of nitrogen-containing heterocycles
• The late-stage C-H functionalization of nitrogen heterocycles
Many nitrogen heterocycles are widely found in natural products, organic materials, agrochemicals, and pharmaceuticals. There are three important areas within heterocyclic chemistry from the perspective of medicinal chemists. Firstly, nature is capable of generating a vast array of complex molecules; to find and evaluate bioactive natural products containing nitrogen heterocycles is critical to the achievement of drug discovery. Secondly, a number of methods to synthesize nitrogen heterocycles are based on the cyclization of acyclic precursors. However, many of these approaches involve the use of expensive/toxic reagents and harsh conditions, hence the continuous need for new and more sustainable synthetic approaches is of particular interest. Lastly, the use of C-H bond functionalization to generate analogues of a sophisticated molecular structure has been identified as an effective strategy; the C-H functionalization of nitrogen heterocycles offers new opportunities in drug discovery. So, the ability to obtain heterocycles with great structural diversity remains an important goal.
More than 75% of drugs approved by the FDA and currently available in the market are nitrogen-containing heterocyclic moieties. In view of this, the goal of this research topic is to highlight recent developments in isolation, construction, and C-H functionalization of nitrogen heterocycles for drug discovery. Research on exploring nitrogen heterocycles from natural resources, such as isolation; structural identification; biological evaluation; and optimization of the extraction process is one of our interests. We also wish to emphasize the importance of novel and efficient synthetic methods and mechanisms for the construction and late-stage modification of nitrogen heterocycles by C-H functionalization.
This Topic welcomes high-quality research including Original Research Articles, Reviews, Mini-Reviews, Perspectives, based on but not limited to the following themes:
• The isolation and structure elucidation of novel nitrogen heterocycles from nature
• Optimization of the extraction process of bioactive nitrogen heterocycles from nature
• Design, synthesis and biological evaluation of nitrogen-containing heterocycles
• Development of new synthetic methods for the construction of nitrogen-containing heterocycles
• The late-stage C-H functionalization of nitrogen heterocycles
