Abstract

As the entire world has been struggling with antimicrobial resistance during the past decades, medicinal chemists have been doing their utmost to tackle this problem through proposing novel scaffolds. According to the estimates, the huge economic burden of antimicrobial resistance has served the issue as a major concern for all societies. It is obvious that we are battling an enemy with weapons that would be ineffective in the near future. Therefore, finding a solution is mandatory before the occurrence of a calamity. Meanwhile, increasing knowledge about the fundamental molecular basis of the drug resistance is required as a key feature for medicinal chemists to rationally design novel anti-microbial agents. In this chapter, we will focus on various antibiotics, including β-lactams, macrolides, aminoglycosides, quinolones, and tetracyclines, discuss the resistance mechanism that each antibiotic is suffering, and introduce novel approaches and synthesized derivatives that would be capable of overcoming the resistance pathways.

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