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Medicinal-Pharmaceutical Chemistry Commons™
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Articles 1 - 6 of 6
Full-Text Articles in Medicinal-Pharmaceutical Chemistry
Design, Synthesis, And Nmr-Guided Characterization Of A Targeted Covalent Inhibitor-Like Molecule Against Ivyp1 From P. Aeruginosa, Samuel Taylor Moore
Design, Synthesis, And Nmr-Guided Characterization Of A Targeted Covalent Inhibitor-Like Molecule Against Ivyp1 From P. Aeruginosa, Samuel Taylor Moore
Master's Theses
Multi-drug resistance poses a serious threat to future generations and historical antibiotic pipelines; consequently, the medical and economic burdens associated with treating multidrug-resistant bacteria are substantiated. In this context, P. aeruginosa (PA) emerges as one of the most significant healthcare challenges, being a leading cause of resistance-associated mortality worldwide. Despite modern efforts to combat these poor outcomes, drug-resistant cases continue to rise, and the need for novel antibiotic treatment is apparent. To this end, we investigated relevant resistance mechanisms and past antibiotic targets within PA, and in doing so, we identified relationships between peptidoglycan biology and a periplasmic protein, Inhibitor …
Methionyl-Trna Synthetase Synthetic And Proofreading Activities Are Determinants Of Antibiotic Persistence, Whitney N. Wood, Miguel Angel Rubio, Lorenzo Eugenio Leiva, Gregory J. Phillips, Michael Ibba
Methionyl-Trna Synthetase Synthetic And Proofreading Activities Are Determinants Of Antibiotic Persistence, Whitney N. Wood, Miguel Angel Rubio, Lorenzo Eugenio Leiva, Gregory J. Phillips, Michael Ibba
Biology, Chemistry, and Environmental Sciences Faculty Articles and Research
Bacterial antibiotic persistence is a phenomenon where bacteria are exposed to an antibiotic and the majority of the population dies while a small subset enters a low metabolic, persistent, state and are able to survive. Once the antibiotic is removed the persistent population can resuscitate and continue growing. Several different molecular mechanisms and pathways have been implicated in this phenomenon. A common mechanism that may underly bacterial antibiotic persistence is perturbations in protein synthesis. To investigate this mechanism, we characterized four distinct metG mutants for their ability to increase antibiotic persistence. Two metG mutants encode changes near the catalytic site …
Metabolic Changes Associated With Adaptive Resistance To Daptomycin In Streptococcus Mitis-Oralis, Allison Parrett, Joseph M. Reed, Stewart G. Gardner, Nagendra N. Mishra, Arnold S. Bayer, Robert Powers, Greg A. Somerville
Metabolic Changes Associated With Adaptive Resistance To Daptomycin In Streptococcus Mitis-Oralis, Allison Parrett, Joseph M. Reed, Stewart G. Gardner, Nagendra N. Mishra, Arnold S. Bayer, Robert Powers, Greg A. Somerville
Department of Chemistry: Faculty Publications
Background: Viridans group streptococci of the Streptococcus mitis-oralis subgroup are important endovascular pathogens. They can rapidly develop high-level and durable non-susceptibility to daptomycin both in vitro and in vivo upon exposure to daptomycin. Two consistent genetic adaptations associated with this phenotype (i.e., mutations in cdsA and pgsA) lead to the depletion of the phospholipids, phosphatidylglycerol and cardiolipin, from the bacterial membrane. Such alterations in phospholipid biosynthesis will modify carbon flow and change the bacterial metabolic status. To determine the metabolic differences between daptomycin-susceptible and non- susceptible bacteria, the physiology and metabolomes of S. mitis-oralis strains 351 (daptomycin-susceptible) and 351-D10 (daptomycin …
Indole Reverses Intrinsic Antibiotic Resistance By Activating A Novel Dual-Function Importer, Yan Wang, Tian Tian, Jingjing Zhang, Xin Jin, Huan Yue, Xiao-Hua Zhang, Liangcheng Du, Fan Bai
Indole Reverses Intrinsic Antibiotic Resistance By Activating A Novel Dual-Function Importer, Yan Wang, Tian Tian, Jingjing Zhang, Xin Jin, Huan Yue, Xiao-Hua Zhang, Liangcheng Du, Fan Bai
Department of Chemistry: Faculty Publications
Bacterial antibiotic resistance modulation by small signaling molecules is an emerging mechanism that has been increasingly reported in recent years. Several studies indicate that indole, an interkingdom signaling molecule, increases bacterial antibiotic resistance. However, the mechanism through which indole reduces antibiotic resistance is largely unknown. In this study, we demonstrated a novel mechanism for indole-mediated reversal of intrinsic antibiotic resistance in Lysobacter. This reversal was facilitated by a novel BtuD-associated dual-function importer that can transfer both vitamin B12 and antibiotics. Indole stimulated btuD overexpression and promoted efficient absorption of extracellular vitamin B12; meanwhile, the weak selectivity …
A Comparison Of The Efficacy Of Newly-Synthesized Antimicrobial Polymers And A Preview Into Their Interaction With The Bacterial Cell Membrane., Kailey Christman
A Comparison Of The Efficacy Of Newly-Synthesized Antimicrobial Polymers And A Preview Into Their Interaction With The Bacterial Cell Membrane., Kailey Christman
Williams Honors College, Honors Research Projects
Antibiotic-resistant bacteria present an obstacle for physicians and researchers. Over 35,000 people die annually in the U.S. from antibiotic-resistant infections each year. New antibiotics are being developed and studied, and natural products are screened to find potential new antibiotics. In this study, four polymer antibiotics with polyester backbones and peptide functional groups were studied with Escherichia coli and Staphylococcus aureus to determine the polymers’ efficacies on the different bacteria and compare the polymers to each other. Timed fluorescence microscopy experiments were performed to determine how long it takes the antibiotics to compromise the membrane integrity of fluorescently-labelled E. coli. …
The Antibacterial Activity Of Metal Complexes Containing 1, 10-Phenanthroline: Potential As Alternatire Therapeutics In The Era Of Antibiotic Resistance, Livia Viganon, Orla L. Howe, Pauraic Mccarron, Malachy Mccann, Michael Devereux
The Antibacterial Activity Of Metal Complexes Containing 1, 10-Phenanthroline: Potential As Alternatire Therapeutics In The Era Of Antibiotic Resistance, Livia Viganon, Orla L. Howe, Pauraic Mccarron, Malachy Mccann, Michael Devereux
Articles
The “antibiotic era”, characterized by the overuse and misuse of antibiotics, over the last half-century has culminated in the present critical “era of resistance”. The treatment of bacterial infections is challenging because of a decline in the current arsenal of useful antibiotics and the slow rate of new drug development. The discovery of a new gene (mcr-1) in 2015, which enables bacteria to be highly resistant to polymyxins (such as colistin), the last line of antibiotic defence left, heralds a new level of concern as this gene is susceptible to horizontal gene transfer, with alarming potential to be spread between …