Heterocyclic Compounds: Synthesis and Medicinal Chemistry Applications, 2nd Edition

Dear Colleagues,

According to several statistical analyses, a high percentage of drugs or biologically active compounds contain aliphatic or aromatic heterocycles. Such moieties can be an essential part of the pharmacophore (antifungal azoles are an example) or may be used to modify ADME/TOX properties (for instance, piperazines in kinase inhibitors). Heterocycles can be used in drug design following optimization strategies such as bioisosterism or scaffold-hopping; in particular, nitrogen-containing heterocycles can be introduced to provide basic or H-bond-forming groups to improve both the pharmacological and pharmaceutical profiles of the drug candidate. Owing to such wide application, the published synthetic methods are continuously applied and optimized to obtain new derivatives, and new synthetic methods are constantly developed in order to overcome the limitations of existing procedures. In recent times, it has also been possible to obtain heterocycles containing elements largely ignored in medicinal chemistry such as silicon, selenium, phosphorous, or boron, and, in some cases, to obtain drugs, such as vaborbactam, a beta-lactamase inhibitor that has been approved for therapy.

Prof. Dr. Maria Novella Romanelli
Guest Editor

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