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Studies On Antibacterial Activities Of N-Thiolated Β-Lactams And Their Polymeric Nanoparticles Against Mrsa, Jeung-Yeop Shim

USF Tampa Graduate Theses and Dissertations

Methicillin-resistant Staphylococcus Aureus (MRSA) is now the most challenging bacterial pathogen affecting patients in hospitals and in care centers, and has brought on the need to develop new drugs for MRSA. This thesis centers on studies of N-thiolated β-lactams, a new family of potent antibacterial compounds that selectively inhibit the growth of methicillin-resistant Staphylococcus aureus (MRSA).

Chapter 1 describes MRSA in more detail. Chapter 2 outlines experiments on the effect of a fatty ester group (CO₂R) on the C₄-phenyl ring of N-methylthio β-lactams, expecting that attachment of long chain ester moieties might increase the hydrophobicity, …

N-Thiolated Β-Lactams: Chemistry And Biology Of A Novel Class Of Antimicrobial Agents For Mrsa, Timothy E. Long

USF Tampa Graduate Theses and Dissertations

N-Methylthio beta-lactams represent a promising new family of antibacterial agents whose in vitro activity is confined largely to Staphylococcus species, including multidrug-resistant forms of S. aureus. Originally developed in the 1980's for use as synthetic intermediates, N-methylthio beta-lactams have recently been shown in these laboratories to possess intriguing biological properties which are addressed in Chapters I-IV. In terms of the antibacterial activities, the structural features and species specificities exhibited by these compounds are unlike those of any existing family of beta-lactam drugs. The lactams seem to exert their effects intracellularly, requiring passage of the bioactive species through the …