β-Lactam inhibitors targeting nucleophilic cysteine and serine enzymes for antiviral and antibacterial applications

Thesis

β-Lactam antibiotics, which include penicillins, cephalosporins, carbapenems, and monobactams, are the most widely used class of antibacterial agents, and their clinical introduction revolutionised modern medicine. Their therapeutic efficacy stems from the ability to target penicillin-binding proteins (PBPs) by acylating the catalytic nucleophilic serine residue, thereby disrupting bacterial cell wall biosynthesis. The versatility of β-lactams, however, extends well beyond their traditional a...

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Authors: Muntean, D

• DOI: 10.5287/ora-6rjn5eedx
• Type of award: DPhil
• Level of award: Doctoral
• Awarding institution: University of Oxford
• Language: English
• Keywords: nucleophilic cysteine / serine protease inhibition; β-lactam; C6-methoxypenicillins; β-lactamases; penicillin-binding proteins; sulbactam derivatives; penicillin antibiotics; cephalosporin antibiotics; antimicrobial resistance; Mpro; COVID-19; AMR; SARS-CoV-2 main protease; 3CLpro; C2-carboxypenicillins; mechanism-based inhibition; β-lactam-based β-lactamase inhibitors
• Subjects: Chemistry, Organic; Bioorganic chemistry