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Articles 1 - 4 of 4
Full-Text Articles in Life Sciences
Indoline‐6‐Sulfonamide Inhibitors Of The Bacterial Enzyme Dape, Cory T. Reidl, Tahirah K. Heath, Iman Darwish, Rachel M. Torrez, Maxwell Moore, Elliot Gild, Boguslaw P. Nocek, Anna Starus, Richard C. Holz, Daniel P. Becker Ph.D.
Indoline‐6‐Sulfonamide Inhibitors Of The Bacterial Enzyme Dape, Cory T. Reidl, Tahirah K. Heath, Iman Darwish, Rachel M. Torrez, Maxwell Moore, Elliot Gild, Boguslaw P. Nocek, Anna Starus, Richard C. Holz, Daniel P. Becker Ph.D.
Chemistry: Faculty Publications and Other Works
Inhibitors of the bacterial enzyme dapE-encoded N-succinyl-l,l-diaminopimelic acid desuccinylase (DapE; EC 3.5.1.18) hold promise as antibiotics with a new mechanism of action. Herein we describe the discovery of a new series of indoline sulfonamide DapE inhibitors from a high-throughput screen and the synthesis of a series of analogs. Inhibitory potency was measured by a ninhydrin-based DapE assay recently developed by our group. Molecular docking experiments suggest active site binding with the sulfonamide acting as a zinc-binding group (ZBG).
Synthesis And Characterization Of Potential Pharmaceutical Analogs Of A Gvsu Lead Compound: An Investigation Of Antibiotic & Anti-Tumor Activity, Nicole Horne
Student Scholars Day Posters
In support of ongoing anti-microbial & anti-tumor research, analogs of a GVSU lead compound, a derivative of the known telomerase inhibitor BIBR1532, were synthesized. These compounds were submitted for biological analysis to determine pharmacological activity toward the discovery of either an antibiotic that can resist bacterial enzymatic degradation or a chemotherapeutic molecule that can destroy tumor cells without increasing toxicity. The anti-microbial interest in these compounds was based on the fact that they are non-penicillin based antibiotics and display a broad range of efficacy against targeted bacteria, including C. diff & MRSA, with minimal toxicity. These compounds were made via …
The Organic Synthesis Of Anthranilic Acid Derivatives As Potential Active Antibiotics, Paul Chappell
The Organic Synthesis Of Anthranilic Acid Derivatives As Potential Active Antibiotics, Paul Chappell
Student Scholars Day Posters
The objective of this research project was to synthesize multiple derivatives of anthranilic acid. These derivatives will then be tested for antibiotic activity against Staphylococcus aureus and Escherichia coli (E. coli). As bacteria become more resistant to penicillin-based antibiotics, the exploration of anthranilic acid-based antibiotics could serve an important role for future medical use. This research project included data collection via 1H-NMR, 12C-NMR, TLC, MP, and IR to determine purity for biological testing.
Development Of Small Molecule Antibiotics Against A Conserved Rna Gene Regulatory Element In Gram-Positive Bacteria, Ville Yrjö Petteri Väre
Development Of Small Molecule Antibiotics Against A Conserved Rna Gene Regulatory Element In Gram-Positive Bacteria, Ville Yrjö Petteri Väre
Legacy Theses & Dissertations (2009 - 2024)
Bacterial infections and the rise of antibiotic resistance, especially multidrug resistant strains, have generated a clear need for discovery of novel therapeutics. Most antibiotics in use today are derivatives of previous antibiotics to which resistance mechanisms already exist, and traditionally they have a single target: either a protein or rRNA. Gram-positive bacteria regulate the expression of several essential genes or operons using a mechanism called the T-box. The T-box is a structurally conserved riboswitch-like gene regulator in the 5’-untranslated region (UTR) of numerous essential genes of Gram-positive bacteria. T-boxes are stabilized by cognate, unacylated tRNA ligands, allowing the formation of …