Literature DB >> 11459657

3-Arylpiperidines as potentiators of existing antibacterial agents.

A Thorarensen1, A L Presley-Bodnar, K R Marotti, T P Boyle, C L Heckaman, M J Bohanon, P K Tomich, G E Zurenko, M T Sweeney, B H Yagi.   

Abstract

Important resistance patterns in Gram-negative pathogens include active efflux of antibiotics out of the cell via a cellular pump and decreased membrane permeability. A 3-arylpiperidine derivative (1) has been identified by high-throughput assay as a potentiator with an IC(50) approximately 90 microM. This report details the evaluation of the tether length, aryl substitution and the importance of the fluorine on antibiotic accumulation. Evaluation of various tether lengths demonstrated that the two-carbon tethered analogues are optimal. Removal of the fluorine has a modest effect on antibiotic accumulation and the defluorinated analogue 17 is equally potent to the original lead 1.

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Year:  2001        PMID： 11459657     DOI： 10.1016/s0960-894x(01)00330-4

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  9 in total

1.  Selected arylpiperazines are capable of reversing multidrug resistance in Escherichia coli overexpressing RND efflux pumps.

Authors:  Jürgen A Bohnert; Winfried V Kern
Journal:  Antimicrob Agents Chemother       Date:  2005-02       Impact factor: 5.191

Review 2.  The challenge of efflux-mediated antibiotic resistance in Gram-negative bacteria.

Authors:  Xian-Zhi Li; Patrick Plésiat; Hiroshi Nikaido
Journal:  Clin Microbiol Rev       Date:  2015-04       Impact factor: 26.132

3.  Permeability Barrier of Gram-Negative Cell Envelopes and Approaches To Bypass It.

Authors:  Helen I Zgurskaya; Cesar A Löpez; S Gnanakaran
Journal:  ACS Infect Dis       Date:  2015       Impact factor: 5.084

4.  Inhibition of antibiotic efflux in bacteria by the novel multidrug resistance inhibitors biricodar (VX-710) and timcodar (VX-853).

Authors:  Steve Mullin; Nagraj Mani; Trudy H Grossman
Journal:  Antimicrob Agents Chemother       Date:  2004-11       Impact factor: 5.191

Review 5.  Microbial efflux pump inhibition: tactics and strategies.

Authors:  George P Tegos; Mark Haynes; J Jacob Strouse; Mohiuddin Md T Khan; Cristian G Bologa; Tudor I Oprea; Larry A Sklar
Journal:  Curr Pharm Des       Date:  2011       Impact factor: 3.116

6.  Mechanistic Duality of Bacterial Efflux Substrates and Inhibitors: Example of Simple Substituted Cinnamoyl and Naphthyl Amides.

Authors:  Napoleon D'Cunha; Mohammad Moniruzzaman; Keith Haynes; Giuliano Malloci; Connor J Cooper; Enrico Margiotta; Attilio V Vargiu; Muhammad R Uddin; Inga V Leus; Feng Cao; Jerry M Parks; Valentin V Rybenkov; Paolo Ruggerone; Helen I Zgurskaya; John K Walker
Journal:  ACS Infect Dis       Date:  2021-08-11       Impact factor: 5.578

7.  Novel Piperazine Arylideneimidazolones Inhibit the AcrAB-TolC Pump in Escherichia coli and Simultaneously Act as Fluorescent Membrane Probes in a Combined Real-Time Influx and Efflux Assay.

Authors:  Jürgen A Bohnert; Sabine Schuster; Winfried V Kern; Tadeusz Karcz; Agnieszka Olejarz; Aneta Kaczor; Jadwiga Handzlik; Katarzyna Kieć-Kononowicz
Journal:  Antimicrob Agents Chemother       Date:  2016-03-25       Impact factor: 5.191

Review 8.  Efflux pump inhibitors for bacterial pathogens: From bench to bedside.

Authors:  Atin Sharma; Vivek Kumar Gupta; Ranjana Pathania
Journal:  Indian J Med Res       Date:  2019-02       Impact factor: 2.375

9.  Broad spectrum resistance in Helicobacter pylori isolated from gastric biopsies of patients with dyspepsia in Cameroon and efflux-mediated multiresistance detection in MDR isolates.

Authors:  Laure Brigitte Kouitcheu Mabeku; Bertrand Eyoum Bille; Cromwell Tepap Zemnou; Lionel Danny Tali Nguefack; Hubert Leundji
Journal:  BMC Infect Dis       Date:  2019-10-22       Impact factor: 3.090
  9 in total

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