Heterocyclic Scaffolds in Novel Synthetic Antibacterial Agents

Abstract

AbstractThe emergence of antibiotic resistant bacteria is becoming a serious global problem. The situation will look very grim in the near future if proper strategies for tackling this menace are not put in place. The use of synthetic drugs for treating microbial diseases decreased after the discovery and development of antibiotics. A paradigm shift in therapeutics for treating bacterial diseases took place with the discovery of penicillin and subsequent advances in the development of other antibiotics. Of late, the emergence of antibiotic resistant variants of the earlier sensitive bacteria and the emergence vis-a-vis development of new infectious diseases have led to a reduction in the effectiveness of antibiotics against bacterial infection. Various strategies have been and are currently investigated and developed to reduce and/or delay bacterial resistance. Nevertheless, there is a tremendous amount of pressure on the scientists and researchers working in the area of medicinal chemistry to deliver novel antimicrobials. At this juncture, it would be helpful if we revisit the classical approach to drug design. Since heterocyclic scaffolds are present abundantly in natural products, they are good targets for the design and synthesis of novel antimicrobial compounds due to their broad range of biological activities and plentiful applications in the extensive fields of pharmacy. Statistically, 75% of the top 200 branded drugs in the world contain heterocyclic moieties in their structures. They have already provided a platform for the rapid growth of research in the areas of organic, pharmaceutical, analytical, and medicinal chemistry. In this chapter, some elementary information about heterocyclic structures in accordance with their ring sizes and their biological and clinical applications has been discussed with the firm belief that the strategic application of modern chemical synthesis to antibacterial drug discovery might play a critical role in the search for novel alternatives to antibiotics.KeywordsAntibacterial agentsHeterocyclic scaffoldsMDR bacteriaChemotherapyBiofilmsAzirine and aziridine scaffoldsAzetidin-2-one (β-lactam)Furan/pyrrole/thiophenePyrazoleImidazole and benzimidazoleTriazoleQuinolineQuinazolineChloroquineSulfanilamideGram-negative bacterial strainsStreptomycinChlortetracyclinePharmacophores and heterocyclic moieties