Prospects for Antibacterial Discovery and Development

Abstract

The rising prevalence of multidrug-resistant bacteria is an urgent health crisis that can only be countered through renewed investment in the discovery and development of antibiotics. There is no panacea for the antibacterial resistance crisis; instead, a multifaceted approach is called for. In this Perspective we make the case that, in the face of evolving clinical needs and enabling technologies, numerous validated antibacterial targets and associated lead molecules deserve a second look. At the same time, many worthy targets lack good leads despite harboring druggable active sites. Creative and inspired techniques buoy discovery efforts; while soil screening efforts frequently lead to antibiotic rediscovery, researchers have found success searching for new antibiotic leads by studying underexplored ecological niches or by leveraging the abundance of available data from genome mining efforts. The judicious use of “polypharmacology” (i.e., the ability of a drug to alter the activities of multiple targets) can also provide new opportunities, as can the continued search for inhibitors of resistance enzymes with the capacity to breathe new life into old antibiotics. We conclude by highlighting available pharmacoeconomic models for antibacterial discovery and development while making the case for new ones.

Development of antibacterial peptides with efficient antibacterial activity, low toxicity, high membrane disruptive activity and a synergistic antibacterial effect

“…The rising prevalence of resistant bacteria is an urgent health crisis which can only be countered through renewed investment in the discovery and development of new antibacterial drugs. 25 In this work, a series of novel amphiphilic AMPs were designed and synthesized based on the biological characteristics of most natural AMPs (such as the positive charge, amphiphilicity, helicity). The antimicrobial activity, hemolysis and cytotoxicity assays showed that the LP21 lipopeptide showed the strongest antimicrobial effect, low hemolysis and cytotoxicity, and still exhibited enough antibacterial activity in the serum, which endowed LP21 with good drug properties.…”

Six‐Pointed Star Chiral Cobalt Superstructures with Strong Antibacterial Activity

“…Therefore, the development of antibacterial materials that are not prone to drug resistance is of great significance to ensure food safety and human health. [1][2][3][4][5][6] and 1180 nm (g-factor = 0.033). The chiral Co SS exhibited obvious chiral optical activity and paramagnetic properties.…”

“…Therefore, the development of antibacterial materials that are not prone to drug resistance is of great significance to ensure food safety and human health. [ 1–6 ]…”

An Ag2S@ZIF-Van nanosystem for NIR-II imaging of bacterial-induced inflammation and treatment of wound bacterial infection

“…[3][4][5] Further, the lack of accurate diagnosis and effective treatment strategies for bacterial infection in clinical settings is an important reason for the sharp rise in bacterial drug resistance. [6][7][8] To address this challenge, the development of advanced, accurate diagnostic methods and efficient anti-bacterial treatment strategies are needed. 9,10 Common traditional detection techniques for diagnosing bacterial infections in clinical settings, which include positron emission tomography 11 and radioactive labeling, 12 lack sufficient resolution and practicality.…”

“…3–5 Further, the lack of accurate diagnosis and effective treatment strategies for bacterial infection in clinical settings is an important reason for the sharp rise in bacterial drug resistance. 6–8 To address this challenge, the development of advanced, accurate diagnostic methods and efficient anti-bacterial treatment strategies are needed. 9,10…”