Design and Discovery of New Antibacterial Agents: Advances, Perspectives, Challenges

Background: Emerging resistance of bacterial pathogens to clinically used drugs, including not only first-choice but also second- and third-choice drugs, is alarming, but since the 1990s only a modest number of new, first in class, drugs for systemic administration have been marketed for the treatment of bacterial infections. Objective: This article provides a review of recently reported new antibacterial chemotherapeutics approved for clinical practice, antibacterial chemotherapeutics in clinical trials and antibacterial agents under development. Discussion: Antibacterial agents include new antibacterial compounds of used drug classes and new antibacterial agents with a novel mode of action. In addition, particular attention is given to agents decreasing bacterial resistance, i.e. to compounds that do not have significant intrinsic bacteriostatic or bactericidal activity, but in combination with antibacterial drugs are able to restore the effect of these drugs or demonstrate synergistic antibacterial properties together with the drugs. Conclusion: This review is specifically focused on small molecules rather than on peptides and discusses a wide range of various molecular scaffolds.