Search Results - "Folkert Reck"
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Challenges of antibacterial drug discovery
Published in ARKIVOC free online journal of organic chemistry (01-01-2019)Get full text
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A Unified Framework for the Incorporation of Bioorthogonal Compound Exposure Probes within Biological Compartments
Published in ACS chemical biology (19-04-2019)“…Compartmentalization is a crucial facet of many biological systems, and key aspects of cellular processes rely on spatial segregation within the cell. While…”
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Identification of Mutations in the mrdA Gene Encoding PBP2 That Reduce Carbapenem and Diazabicyclooctane Susceptibility of Escherichia coli Clinical Isolates with Mutations in ftsI (PBP3) and Which Carry blaNDM-1
Published in mSphere (2019)“…ABSTRACTPenicillin-binding proteins (PBPs) are essential for bacterial cell wall biosynthesis, and several are clinically validated antibacterial targets of…”
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Inhibitors of the bacterial cell wall biosynthesis enzyme MurC
Published in Bioorganic & medicinal chemistry letters (04-06-2001)“…A series of phosphinate transition-state analogues of the l-alanine adding enzyme (MurC) of bacterial peptidoglycan biosynthesis was prepared and tested as…”
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Scale-Up Synthesis of IID572: A New β‑Lactamase Inhibitor
Published in Organic process research & development (17-07-2020)“…The new potentially best-in-class β-lactamase inhibitor IID572 was discovered by a late-stage functionalization approach. An alternative synthesis was…”
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In Vitro Activity of LYS228, a Novel Monobactam Antibiotic, against Multidrug-Resistant Enterobacteriaceae
Published in Antimicrobial agents and chemotherapy (01-10-2018)“…LYS228 is a novel monobactam with potent activity against LYS228 is stable to metallo-β-lactamases (MBLs) and serine carbapenemases, including carbapenemases…”
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Optimization of novel monobactams with activity against carbapenem-resistant Enterobacteriaceae – Identification of LYS228
Published in Bioorganic & medicinal chemistry letters (15-02-2018)“…[Display omitted] Metallo-β-lactamases (MBLs), such as New Delhi metallo-β-lactamase (NDM-1) have spread world-wide and present a serious threat. Expression of…”
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Mode of Action of the Monobactam LYS228 and Mechanisms Decreasing In Vitro Susceptibility in Escherichia coli and Klebsiella pneumoniae
Published in Antimicrobial agents and chemotherapy (01-10-2018)“…The monobactam scaffold is attractive for the development of new agents to treat infections caused by drug-resistant Gram-negative bacteria because it is…”
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Novel N-Linked Aminopiperidine Inhibitors of Bacterial Topoisomerase Type II: Broad-Spectrum Antibacterial Agents with Reduced hERG Activity
Published in Journal of medicinal chemistry (24-11-2011)“…Novel non-fluoroquinolone inhibitors of bacterial type II topoisomerases (DNA gyrase and topoisomerase IV) are of interest for the development of new…”
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NBTI 5463 Is a Novel Bacterial Type II Topoisomerase Inhibitor with Activity against Gram-Negative Bacteria and In Vivo Efficacy
Published in Antimicrobial agents and chemotherapy (01-05-2014)“…The need for new antibiotics that address serious Gram-negative infections is well recognized. Our efforts with a series of novel bacterial type II…”
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Topoisomerase Inhibitors Addressing Fluoroquinolone Resistance in Gram-Negative Bacteria
Published in Journal of medicinal chemistry (23-07-2020)“…Since their discovery over 5 decades ago, quinolone antibiotics have found enormous success as broad spectrum agents that exert their activity through dual…”
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Novel N-Linked Aminopiperidine Inhibitors of Bacterial Topoisomerase Type II with Reduced pK a: Antibacterial Agents with an Improved Safety Profile
Published in Journal of medicinal chemistry (09-08-2012)“…Novel non-fluoroquinolone inhibitors of bacterial type II topoisomerases (DNA gyrase and topoisomerase IV) are of interest for the development of new…”
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Impact of Inducible bla DHA-1 on Susceptibility of Klebsiella pneumoniae Clinical Isolates to LYS228 and Identification of Chromosomal mpl and ampD Mutations Mediating Upregulation of Plasmid-Borne bla DHA-1 Expression
Published in Antimicrobial agents and chemotherapy (01-10-2018)“…Twenty-three ( ) clinical isolates exhibited a range of susceptibilities to LYS228, with MICs of ≥8 μg/ml for 9 of these. Mutants with decreased susceptibility…”
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Impact of Inducible blaDHA-1 on Susceptibility of Klebsiella pneumoniae Clinical Isolates to LYS228 and Identification of Chromosomal mpl and ampD Mutations Mediating Upregulation of Plasmid-Borne blaDHA-1 Expression
Published in Antimicrobial agents and chemotherapy (24-09-2018)“…Twenty-three Klebsiella pneumoniae (blaDHA-1) clinical isolates exhibited a range of susceptibilities to LYS228, with MICs of ≥8 μg/ml for 9 of these. Mutants…”
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Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria
Published in Journal of medicinal chemistry (13-05-2021)“…Herein, we describe the discovery and optimization of a novel series that inhibits bacterial DNA gyrase and topoisomerase IV via binding to, and stabilization…”
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Synthesis of ciprofloxacin dimers for evaluation of bacterial permeability in atypical chemical space
Published in Bioorganic & medicinal chemistry letters (01-09-2015)“…[Display omitted] We describe the synthesis and evaluation of a library of variably-linked ciprofloxacin dimers. These structures unify and expand on the use…”
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Identification of 4-Substituted 1,2,3-Triazoles as Novel Oxazolidinone Antibacterial Agents with Reduced Activity against Monoamine Oxidase A
Published in Journal of medicinal chemistry (27-01-2005)“…Oxazolidinones represent a new and promising class of antibacterial agents. Current research in this area is mainly concentrated on improving the safety…”
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Target-based resistance in Pseudomonas aeruginosa and Escherichia coli to NBTI 5463, a novel bacterial type II topoisomerase inhibitor
Published in Antimicrobial agents and chemotherapy (01-01-2015)“…In a previous report (T. J. Dougherty, A. Nayar, J. V. Newman, S. Hopkins, G. G. Stone, M. Johnstone, A. B. Shapiro, M. Cronin, F. Reck, and D. E. Ehmann,…”
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Exploring Left-Hand-Side substitutions in the benzoxazinone series of 4-amino-piperidine bacterial type IIa topoisomerase inhibitors
Published in Bioorganic & medicinal chemistry letters (15-09-2011)“…An SAR survey at the C-6 benzoxazinone position of a novel scaffold which inhibits bacterial type IIa topoisomerase demonstrates that a range of small electron…”
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