Start Date
2018
Description
Bacterial resistance continues to be a growing threat throughout the world. In the US alone, 2 million people are infected by, and 23,000 die from antibiotic-resistant bacteria each year. 1 Developing antibiotics to treat infections caused by Gram-negative and Gram-positive bacteria has become the focus of research efforts worldwide. Fluoroquinolones are a large, marketed class of antimicrobial agents that are effective against both types of bacteria. They target DNA Gyrase and Topoisomerase IV, type II topoisomerase enzymes that are involved in DNA replication, specifically negative supercoiling and decatenation, respectively.
As fluoroquinolones have been clinically used since the mid 80’s, their usefulness has eroded due the development of bacterial resistance. 2 The need for novel derivatives that engage new residues in the binding complex (see red shaded area) is a principal focus of this project.
Recommended Citation
Biel, Sara and Barbachyn, Michael, "Progress Toward the Synthesis of Novel Bacterial Topoisomerase Inhibitors Derived from Fluoroquinolones. N-1 Alkyne Derivaties" (2018). Summer Research. 12.
https://digitalcommons.calvin.edu/summer_research/2018/Posters/12
Included in
Progress Toward the Synthesis of Novel Bacterial Topoisomerase Inhibitors Derived from Fluoroquinolones. N-1 Alkyne Derivaties
Bacterial resistance continues to be a growing threat throughout the world. In the US alone, 2 million people are infected by, and 23,000 die from antibiotic-resistant bacteria each year. 1 Developing antibiotics to treat infections caused by Gram-negative and Gram-positive bacteria has become the focus of research efforts worldwide. Fluoroquinolones are a large, marketed class of antimicrobial agents that are effective against both types of bacteria. They target DNA Gyrase and Topoisomerase IV, type II topoisomerase enzymes that are involved in DNA replication, specifically negative supercoiling and decatenation, respectively.
As fluoroquinolones have been clinically used since the mid 80’s, their usefulness has eroded due the development of bacterial resistance. 2 The need for novel derivatives that engage new residues in the binding complex (see red shaded area) is a principal focus of this project.