Designing New Antimicrobials Based on Known Valuable Heterocycles as Building Blocks

Dear Colleagues,

Heterocycles are essential structural components in various antimicrobial drugs. The significance of heterocycles in drug design resides in their ability to modify the drug candidate’s physicochemical characteristics, biological impact, and pharmacokinetic and toxicological profile. Numerous recent studies have targeted therapeutic agents with heterocycle-based structures. In the last decade, diverse heterocyclic compounds have been synthesized to develop new antimicrobials capable of treating bacterial, viral, fungal, or parasitic infections. The physicochemical properties imparted by a heterocycle are associated with the biological activity of the drug (the spectrum of activity and potency) and its pharmacokinetic, pharmacologic, and toxicological profiles. Highlighting the relationships between heterocycles in the molecular structure of antimicrobial drugs and their biological properties can serve as the basis for many other rational design studies for discovering new antimicrobials (antibiotics, antivirals, antifungals, and antiparasitics). Incorporating valuable heterocycles into the molecular structure of antimicrobials represents a promising avenue for advancing drug development. It offers opportunities to enhance drug efficacy, safety, and diversity, which is crucial in the ongoing battle with infections, parasitosis, and resistance to antimicrobials. As a result of drug resistance in bacteria, fungi, HIV, tuberculosis, malaria, and tropical diseases, antibiotics and other antimicrobial drugs become ineffective, and infections become difficult or impossible to treat, increasing the risk of disease, severe illness, disability, and death.

This Topic focuses on the rational design of novel antimicrobials by leveraging the structural diversity and pharmacological potential of known valuable heterocycles as fundamental building blocks. Continued research is essential to translate all promising findings into effective treatments that benefit global public health. The proposed Topic aims to identify the latest trends in discovering new antimicrobials based on valuable heterocycles as building blocks and will welcome both research papers and reviews.

Prof. Dr. Aura Rusu
Prof. Dr. Gabriel Hancu
Dr. Vladimír Garaj
Topic Editors