The article analyzes synthetic strategies, antibacterial activities, and structure-activity relationships for various derivatives of nitrogen-heterocyclic antibacterial agents, including pyrazole, imidazole, triazole, thiazole, indole, and quinolone to promote clinical translation of nitrogen-heterocyclic antibacterial candidate drugs.
Abstract
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.
The alarming rise of life-threatening microbial infections has intensified the search for novel broad-spectrum antimicrobial agents. Imidazole, a versatile nitrogen-containing heterocycle, has emerged as a privileged scaffold due to its diverse biological activities, including antibacterial, antifungal, and anticancer...
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INTRODUCTION
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