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Your search keyword '"Mark J. Mitton-Fry"' showing total 6 results
Start Over Author "Mark J. Mitton-Fry" Journal bioorganic & medicinal chemistry letters
6 results on '"Mark J. Mitton-Fry"'

1. Synthesis and anti-staphylococcal activity of novel bacterial topoisomerase inhibitors with a 5-amino-1,3-dioxane linker moiety

Author

Mark J. Mitton-Fry, Zoe Li, Soumendrakrishna Karmahapatra, Sheri Dellos-Nolan, Jack C. Yalowich, Linsen Li, Antony A. Okumu, Daniel J. Wozniak, and Anthony English

Subjects
Methicillin-Resistant Staphylococcus aureus, Models, Molecular, 0301 basic medicine, Stereochemistry, medicine.drug_class, 030106 microbiology, Clinical Biochemistry, hERG, Pharmaceutical Science, Microbial Sensitivity Tests, Crystallography, X-Ray, medicine.disease_cause, Biochemistry, DNA gyrase, Dioxanes, Structure-Activity Relationship, 03 medical and health sciences, Drug Discovery, Potassium Channel Blockers, medicine, Humans, Topoisomerase II Inhibitors, Structure–activity relationship, Molecular Biology, Dose-Response Relationship, Drug, Molecular Structure, biology, Chemistry, Topoisomerase, Organic Chemistry, Ether-A-Go-Go Potassium Channels, Anti-Bacterial Agents, DNA Topoisomerases, Type II, 030104 developmental biology, Staphylococcus aureus, Quinolines, biology.protein, Molecular Medicine, Topoisomerase-II Inhibitor, Type II topoisomerase, Topoisomerase inhibitor
Abstract

Novel bacterial type II topoisomerase inhibitors (NBTIs) constitute a promising new class of antibacterial agents. We report a series of NBTIs with potent anti-staphylococcal activity and diminished hERG inhibition. Dioxane-linked compound 9 demonstrated MICs ≤1 μg/mL against both methicillin-susceptible (MSSA) and -resistant Staphylococcus aureus (MRSA), accompanied by reduced hERG inhibition as compared to cyclohexane- or piperidine-linked analogs.

Published
2018

2. Heterocyclic methylsulfone hydroxamic acid LpxC inhibitors as Gram-negative antibacterial agents

Author

Lisa Mullins, Daniel P. Uccello, Justin I. Montgomery, Ye Che, John P. O'Donnell, Mark S. Plummer, Joseph A. Abramite, Seung Won Chung, Loren M. Price, Mark C. Noe, Laura A. McAllister, Rose Barham, Mark J. Mitton-Fry, Andrew P. Tomaras, Usa Reilly, Matthew Frank Brown, Jinshan M. Chen, Joseph Penzien, Carol A. Menard, Veerabahu Shanmugasundaram, and Robert M. Oliver

Subjects
Gram-negative bacteria, Klebsiella pneumoniae, Clinical Biochemistry, Pharmaceutical Science, Microbial Sensitivity Tests, Hydroxamic Acids, Biochemistry, Amidohydrolases, Structure-Activity Relationship, chemistry.chemical_compound, Heterocyclic Compounds, Gram-Negative Bacteria, Drug Discovery, Structure–activity relationship, Sulfones, Enzyme Inhibitors, Molecular Biology, chemistry.chemical_classification, Hydroxamic acid, biology, Organic Chemistry, biology.organism_classification, Anti-Bacterial Agents, Enzyme, chemistry, Pseudomonas aeruginosa, Molecular Medicine, Antibacterial activity, Bacterial outer membrane, Bacteria
Abstract

The synthesis and antibacterial activity of heterocyclic methylsulfone hydroxamates is presented. Compounds in this series are potent inhibitors of the LpxC enzyme, a key enzyme involved in the production of lipopolysaccharide (LPS) found in the outer membrane of Gram-negative bacteria. SAR evaluation of compounds in this series revealed analogs with potent antibacterial activity against challenging Gram-negative species such as Pseudomonas aeruginosa and Klebsiella pneumoniae.

Published
2012

3. Novel monobactams utilizing a siderophore uptake mechanism for the treatment of gram-negative infections

Author

Hongying Gao, Jennifer A. Young, Joel R. Hardink, Veerabahu Shanmugasundaram, Steven M. Finegan, David Pattavina, Joel T. Arcari, Jian Lin, Jianmin Sun, Mark J. Mitton-Fry, Thuy Hoang, Matthew Frank Brown, Hud Lawrence Risley, Rebecca Irvine, Mark Edward Flanagan, Brandon P. Schuff, Seungil Han, Manjinder S. Lall, Brian S. Gerstenberger, Mark Niosi, Thomas M. Harris, Michael D. Huband, Chao Li, Lisa Mullins, Sandra P. McCurdy, M. Megan Lemmon, John P. Mueller, Jennifer Winton, Jeffrey M. Casavant, Mark S. Plummer, Mark C. Noe, Joseph Penzien, Jeremy T. Starr, and David M. George

Subjects
Models, Molecular, Siderophore, Klebsiella pneumoniae, Clinical Biochemistry, Pharmaceutical Science, Microbial Sensitivity Tests, Crystallography, X-Ray, medicine.disease_cause, Biochemistry, Microbiology, Mice, Structure-Activity Relationship, In vivo, Drug Resistance, Multiple, Bacterial, Gram-Negative Bacteria, Drug Discovery, medicine, Animals, Humans, Monobactam, Monobactams, Molecular Biology, Escherichia coli, Binding Sites, Dose-Response Relationship, Drug, Molecular Structure, biology, Chemistry, Pseudomonas aeruginosa, Organic Chemistry, Blood Proteins, biology.organism_classification, In vitro, Rats, Molecular Medicine, Gram-Negative Bacterial Infections, medicine.drug
Abstract

Novel siderophore-linked monobactams with in vitro and in vivo anti-microbial activity against MDR Gram-negative pathogens are described.

Published
2012

4. Structure–activity relationships and hepatic safety risks of thiazole agonists of the thrombopoietin receptor

Author

James P. Driscoll, Eric B. McElroy, Christopher S. Jones, Matthew Frank Brown, Jonathan L. Doty, William H. Brissette, Sharon L. Ripp, Mark J. Mitton-Fry, Marc I. Smeets, Thomas M. Harris, Kristen A. Trevena, Amy S. Antipas, Jeffrey M. Casavant, Laura Cook Blumberg, David A. Reim, Lawrence A. Reiter, Michael John Munchhof, Sandra P. McCurdy, and Andrei Shavnya

Subjects
Agonist, medicine.drug_class, Clinical Biochemistry, Pharmaceutical Science, Pharmacology, Biochemistry, Structure-Activity Relationship, chemistry.chemical_compound, Aminothiazole, Drug Discovery, medicine, Animals, Structure–activity relationship, Receptor, Thiazole, Molecular Biology, Thrombopoietin, Thrombopoietin receptor, Organic Chemistry, In vitro, Thiazoles, Liver, chemistry, Molecular Medicine, Receptors, Thrombopoietin
Abstract

5-F substitution of an aminothiazole moiety within a series of thrombopoietin receptor agonists leads to potent agents with an improved hepatic safety profile in rodent toxicology studies.

Published
2010

5. The identification of orally bioavailable thrombopoietin agonists

Author

Lilli Ann Wolf-Gouveia, Paul D. Lira, Eric B. McElroy, Lisa Marie Thomasco, Matthew Frank Brown, Christopher S. Jones, Jonathan L. Doty, Lawrence A. Reiter, Sandra P. McCurdy, Anthony Marfat, Sharon L. Ripp, Mark J. Mitton-Fry, William H. Brissette, Andrei Shavnya, Linde Robert Gerald, Thomas M. Harris, Kristen A. Trevena, Qifang Li, Laura Cook Blumberg, Amy S. Antipas, James P. Driscoll, Michael John Munchhof, and Jeffrey M. Casavant

Subjects
Agonist, Pyrimidine, medicine.drug_class, Clinical Biochemistry, Administration, Oral, Biological Availability, Pharmaceutical Science, Pharmacology, Benzoates, Biochemistry, chemistry.chemical_compound, Piperidines, Pharmacokinetics, In vivo, Drug Discovery, medicine, Animals, Humans, Moiety, Benzamide, Molecular Biology, Thrombopoietin, Organic Chemistry, Pyrazinamide, Rats, Bioavailability, Hydrazines, Pyrimidines, chemistry, Pyrazoles, Molecular Medicine, Caco-2 Cells, Receptors, Thrombopoietin
Abstract

Recently, we disclosed a series of potent pyrimidine benzamide-based thrombopoietin receptor agonists. Unfortunately, the structural features required for the desired activity conferred physicochemical properties that were not favorable for the development of an oral agent. The physical properties of the series were improved by replacing the aminopyrimidinyl group with a piperidine-4-carboxylic acid moiety. The resulting compounds possessed favorable in vivo pharmacokinetic properties, including good bioavailability.

Published
2009

6. Corrigendum to 'Novel monobactams utilizing a siderophore uptake mechanism for the treatment of Gram-negative infections' [Bioorg. Med. Chem. Lett. 22/18 (2012) 5989–5994]

Author

Chao Li, Mark S. Plummer, Veerabahu Shanmugasundaram, Thuy Hoang, Seungil Han, Lisa Mullins, Jennifer A. Young, Mark C. Noe, Thomas M. Harris, Steven M. Finegan, John P. Mueller, Joel R. Hardink, Jian Lin, Joel T. Arcari, Hongying Gao, Jennifer Winton, Manjinder S. Lall, Jeffrey M. Casavant, Jianmin Sun, Hud Lawrence Risley, Mark Edward Flanagan, Joseph Penzien, Brandon P. Schuff, Mark Niosi, Brian S. Gerstenberger, Mark J. Mitton-Fry, Jeremy T. Starr, Rebecca Irvine, David M. George, Matthew Frank Brown, M. Megan Lemmon, Sandra P. McCurdy, Michael D. Huband, and David Pattavina

Subjects
Siderophore, Mechanism (biology), Chemistry, Stereochemistry, Organic Chemistry, Clinical Biochemistry, Drug Discovery, Pharmaceutical Science, Molecular Medicine, Monobactams, Molecular Biology, Biochemistry, Gram
Published
2015

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