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Literature DB >> 30740245

Nitro Sulfonyl Fluorides are a new pharmacophore for the development of antibiotics.

Corinne Sadlowski^1,2, Bora Park^1,2, Clarissa Araújo³, Subhamoy Das¹, D Lucas Kerr¹, Maomao He¹, Hesong Han¹, Lee Riley³, Niren Murthy¹.

Abstract

The development of antibiotics against Gram-negative bacteria is a central problem in drug discovery. In this report, we demonstrate that aromatic sulfonyl fluorides with a nitro group in their ortho position have remarkable antibacterial activity and are active against drug-resistant pathogens, such as methicillin-resistant Staphylococcus aureus (MRSA), multidrug resistant Acinetobacter baumannii, and Pseudomonas aeruginosa.

Entities: Chemical Disease Gene Species

Year: 2018 PMID： 30740245 PMCID： PMC6366622 DOI： 10.1039/C8ME00011E

Source DB: PubMed Journal: Mol Syst Des Eng

17 in total

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Authors: M Solomon; B Belenghi; M Delledonne; E Menachem; A Levine
Journal: Plant Cell Date: 1999-03 Impact factor: 11.277

Review 2. Irreversible inhibitors of serine, cysteine, and threonine proteases.

Authors: James C Powers; Juliana L Asgian; Ozlem Dogan Ekici; Karen Ellis James
Journal: Chem Rev Date: 2002-12 Impact factor: 60.622

3. Strategies for discovering and derisking covalent, irreversible enzyme inhibitors.

Authors: Douglas S Johnson; Eranthie Weerapana; Benjamin F Cravatt
Journal: Future Med Chem Date: 2010-06 Impact factor: 3.808

Review 4. Drug discovery considerations in the development of covalent inhibitors.

Authors: Robert Mah; Jason R Thomas; Cynthia M Shafer
Journal: Bioorg Med Chem Lett Date: 2013-10-10 Impact factor: 2.823

5. Cell sensitivity assays: the MTT assay.

Authors: Johan van Meerloo; Gertjan J L Kaspers; Jacqueline Cloos
Journal: Methods Mol Biol Date: 2011

6. Towards an informative mutant phenotype for every bacterial gene.

Authors: Adam Deutschbauer; Morgan N Price; Kelly M Wetmore; Daniel R Tarjan; Zhuchen Xu; Wenjun Shao; Dacia Leon; Adam P Arkin; Jeffrey M Skerker
Journal: J Bacteriol Date: 2014-08-11 Impact factor: 3.490

7. Structural and mechanistic studies of Escherichia coli nitroreductase with the antibiotic nitrofurazone. Reversed binding orientations in different redox states of the enzyme.

Authors: Paul R Race; Andrew L Lovering; Richard M Green; Abdelmijd Ossor; Scott A White; Peter F Searle; Christopher J Wrighton; Eva I Hyde
Journal: J Biol Chem Date: 2005-01-31 Impact factor: 5.157

Review 8. Burden of endemic health-care-associated infection in developing countries: systematic review and meta-analysis.

Authors: Benedetta Allegranzi; Sepideh Bagheri Nejad; Christophe Combescure; Wilco Graafmans; Homa Attar; Liam Donaldson; Didier Pittet
Journal: Lancet Date: 2010-12-09 Impact factor: 79.321

Nitro Sulfonyl Fluorides are a new pharmacophore for the development of antibiotics.

1. The involvement of cysteine proteases and protease inhibitor genes in the regulation of programmed cell death in plants.

Review 2. Irreversible inhibitors of serine, cysteine, and threonine proteases.

3. Strategies for discovering and derisking covalent, irreversible enzyme inhibitors.

Review 4. Drug discovery considerations in the development of covalent inhibitors.

5. Cell sensitivity assays: the MTT assay.

6. Towards an informative mutant phenotype for every bacterial gene.

7. Structural and mechanistic studies of Escherichia coli nitroreductase with the antibiotic nitrofurazone. Reversed binding orientations in different redox states of the enzyme.

Review 8. Burden of endemic health-care-associated infection in developing countries: systematic review and meta-analysis.

Review 9. Bioactivation and hepatotoxicity of nitroaromatic drugs.

Review 10. Reduction of polynitroaromatic compounds: the bacterial nitroreductases.

1. SuFEx-enabled, agnostic discovery of covalent inhibitors of human neutrophil elastase.

2. Facile one-pot synthesis of sulfonyl fluorides from sulfonates or sulfonic acids.

3. Nitrofurans: Revival of an "old" drug class in the fight against antibiotic resistance.