Development of Bacterial Quorum Sensing Inhibitors and Molecular Probes

Author

Hanjing Peng, Georgia State UniversityFollow

Date of Award

Fall 12-26-2012

Degree Type

Dissertation

Degree Name

Doctor of Philosophy (PhD)

Department

Chemistry

First Advisor

Binghe Wang

Abstract

Bacterial quorum sensing is regarded as a novel target for the design of antimicrobials. Based on lead structures identified from HTS, 39 analogues have been synthesized and evaluated in Vibrio haveyi. Potent inhibitors with IC₅₀ values at single-digit micromolar concentrations for AI-2 mediated quorum sensing have been identified. On the second project, post-synthesis modifications of DNA provide easy functionalizations for expanded applications such as aptamer selection. A CBT-modified thymidine analogue (CBT-TTP) has been synthesized and used for enzymatic incorporation into DNA. Post-synthesis modifications through condensation with 1,2-aminothiol for installation of a boronic acid moiety or a fluorophore have been achieved. On the third project, H₂S has been recognized as an important gasotransmitter and its concentration is relevant to a variety of diseases. A novel fluorescent probe (DNS-Az) has been developed for quantitation of H₂S in aqueous solutions. This probe has been used to measure H₂S concentrations in the blood.

DOI

https://doi.org/10.57709/3490218

Recommended Citation

Peng, Hanjing, "Development of Bacterial Quorum Sensing Inhibitors and Molecular Probes." Dissertation, Georgia State University, 2012.
doi: https://doi.org/10.57709/3490218