Abstract
Bedquiline (BDQ), a novel antibiotic, significantly inhibits the F0 c-ring of F-ATP synthase (F-ATPase) in drug resistant M. tuberculosis through steric hindrance and stops ATP production, thereby facilitating cell death However, due to differences in amino acid sequence, binding affinity of BDQ to the F-ATP synthases of other bacteria are significantly reduced. Primarily targeting Gram-negative E. coli, analogs of BDQ were synthesized to determine the efficacy of distinct functional groups to create the most potent analog. By changing the position of the hydroxy group to C1 instead of C2, to account for the changes at amino acid position 65 – Glu65→Asp65, it is theorized that binding will be enhanced. Synthesized analogs’ potency were determined via inside-out vesicle H+ pumping and bacterial assays.
How to Cite
Hanamean, A. M., (2018) “Synthesis and Antibiotic Evaluation of Bedaquiline Analogs in Complex with E. coli’s Gram-Negative F1F0-ATP Synthase”, Capstone, The UNC Asheville Journal of Undergraduate Scholarship 31(2), 5/1/2019.
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