Globalink research award: Thematics call

Herein, we propose the lead optimization of novel antitubercular quinolone compounds targeting the DprE1 enzyme; an important enzyme in Mtb cell wall biosynthesis. The previously synthesised compounds exhibited sub-micromolar activity against the wild type (H37Rv) Mycobacterium (Mtb) strain. The lead compound in the series further exhibited activity against resistant fluoroquinolone Mtb strains and it binding affinity proved to be similar to the current DprE1 suicide inhibitors drugs. Unfortunately when the the ADME properties of these compounds were evaluated, they displayed poor aqueous solubility and metabolic stability. Thus, we herein propose optimization of the previously identified molecules by appending different groups at C-3 of the quinolone nucleus to improve aqueous solubility and metabolic stability.

Faculty Supervisor:

David MaGee

Student:

Partner:

North-West University

Discipline:

Life Sciences

Sector:

Pharmaceuticals

University:

University of New Brunswick

Program: