Recent Progress in Organic Small‐Molecule Antibacterial Agents

Antibiotic resistance has become a critical global threat, creating an urgent need for new antibacterial agents. Among therapeutic modalities, small-molecule antibacterials offer significant advantages, including controllable metabolism and flexible structural design, making them an excellent platform for combating drug-resistant bacteria. This review highlights recent progress in organic small-molecule antibacterials and is organized into three sections: antibiotics, natural products and their derivatives, and other synthetic small-molecule agents (including heterocyclic, sulfonamide, and amphiphilic compounds). Each section summarizes recent advances in the field, and the review concludes by discussing future directions and challenges in small-molecule antibiotic development. By drawing on strategies across these categories, this overview provides researchers in the field with a fresh perspective to inspire novel approaches and accelerate the development of new antibacterial drugs.