New compounds for a good old class: Synthesis of two Β-lactam bearing cephalosporins and their evaluation with a multidisciplinary approach.

摘要: Antimicrobial resistance is spreading massively in the world and becoming one of main health threats 21st century. One possible strategies to overcome this problem modify known classes antibiotics a rational way, with aim tuning their efficacy. In paper, we present synthesis evaluation biological activity series two β-lactam bearing cephalosporin derivatives, which an additional isolated azetidinone ring, different substituents, joined classical cephalosporanic nucleus by chain variable length. A computational approach has been also applied order predict molecular interactions between some representative derivatives selected penicillin-binding proteins, natural targets antibiotics. All these are active against Gram-positive bacteria, MIC100 comparable or even better than that reference antibiotic ceftriaxone, show no very low cytotoxic on cell lines. Overall, molecules appear be able exert particular microorganisms belonging species more involved development multidrug resistance.