Synthesis of aza-tetracyclic indolines for the treatment of Methicillin-resistant Staphylococcus aureus

Undergraduate Honors Thesis

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Citeable URL: https://scholar.colorado.edu/concern/undergraduate_honors_theses/000000485

Abstract

Antibiotic resistance is a major threat to public health. Currently new multi-drug resistant bacterial strains are appearing faster than new antibiotics can enter the clinic. Resistance modifying agents can potentially potentiate whole families of antibiotics and are one way to combat antibiotic resistance. Previously, our lab synthesized a library of polycyclic indolines which were found to potentiate β-lactams in MRSA in vitro but were poor candidates for in vivo testing due to their physical properties. To improve their physical properties, we synthesized a small library of aza-tetracyclic indolines. The nitrogen was functionalized with various functional groups to determine which modifications are tolerated at that position. One methyl carbamate aza-tetracyclic indoline has improved physical properties compared to its lead compound, while still maintaining β-lactam potentiating activity in MRSA.

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