Nitrogen-Containing Heterocycles in Antibacterial Drug Discovery: Recent Advances and Structure-Activity Relationships.

Antibiotic resistance has become a major global public health challenge, creating an urgent need for the development of new antimicrobial agents. This article reviews the latest research on nitrogen-heterocyclic antimicrobial agents, including pyrazole, imidazole, triazole, thiazole, indole, and quinolone. The article analyzes synthetic strategies, antibacterial activities, and structure-activity relationships for various derivatives. Eight key antibacterial scaffolds, namely compounds 21aa, 30a, 40, 63S, 91, 105, 123, and 127a, were identified as exhibiting outstanding performance. Future research should focus on evaluating the in vivo pharmacodynamics, pharmacokinetics, clinical translation challenges, and safety of these key antibacterial scaffolds, thereby promoting the clinical translation of nitrogen-heterocyclic antibacterial candidate drugs.