Design, Syntheses and Biological Evaluation of Novel Cephalosporin and Oxazolidinone-Based Antibiotics

The research in this thesis involved two main projects that focus on the development of novel antibiotics to overcome bacterial resistance problem. The first project involved the syntheses and biological evaluation of cephalosporin and oxazolidinone-based antibiotics using nitroso DielsÌ¢‰âÂ'Alder and related chemistry. The second main project involved the syntheses and biological studies of cephalosporin-oxazolidinone dual action prodrugs. In Chapter 1, the synthesis of cephalosporin-based antibiotics using nitroso DielsÌ¢‰âÂ'Alder chemistry was rationalized and described. Chapter 2 described the synthesis of novel oxazine and aminocycloalkenol containing oxazolidinone antibiotics using nitroso DielsÌ¢‰âÂ'Alder chemistry. In addition, in vitro antibacterial studies were included. In chapter 3, cephalosporin-oxazolidinone multifunctional compounds were rationally designed and synthesized. Their stability in aqueous media in the presence of Beta-lactamase and in vitro antimicrobial activity were investigated