Literature DB >> 18848780

Piperine analogs as potent Staphylococcus aureus NorA efflux pump inhibitors.

Payare L Sangwan1, Jawahir L Koul, Surrinder Koul, Mallepally V Reddy, Niranjan Thota, Inshad A Khan, Ashwani Kumar, Nitin P Kalia, Ghulam N Qazi.   

Abstract

Based on our recent findings that piperine is a potent Staphylococcus aureus NorA efflux pump inhibitor (EPI), 38 piperine analogs were synthesized and bioevaluated for their EPI activity. Twenty-five of them were found active with potentiating activity equivalent or more than known EPIs like reserpine, carsonic acid and verapamil. The inhibitory mechanism of the compounds was confirmed by efflux inhibition assay using ethidium bromide as NorA substrate. The present communication describes the synthesis, bioevaluation and structure related activity of these efflux pump inhibitors.

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Year:  2008        PMID: 18848780     DOI: 10.1016/j.bmc.2008.09.042

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  17 in total

Review 1.  Efflux-mediated drug resistance in bacteria: an update.

Authors:  Xian-Zhi Li; Hiroshi Nikaido
Journal:  Drugs       Date:  2009-08-20       Impact factor: 9.546

2.  Advances in the structural studies of antibiotic potentiators against Escherichia coli.

Authors:  Gifty A Blankson; Ajit K Parhi; Malvika Kaul; Daniel S Pilch; Edmond J LaVoie
Journal:  Bioorg Med Chem       Date:  2019-06-04       Impact factor: 3.641

3.  Inhibition of Invasion in Pancreatic Cancer Cells by Conjugate of EPA with β(3,3)-Pip-OH via PI3K/Akt/NF-kB Pathway.

Authors:  Hina Amin; Naiem Ahmad Wani; Saleem Farooq; Debasis Nayak; Souneek Chakraborty; Sudha Shankar; Reyaz Ur Rasool; Surinder Koul; Anindya Goswami; Rajkishor Rai
Journal:  ACS Med Chem Lett       Date:  2015-08-31       Impact factor: 4.345

Review 4.  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

5.  Structure-activity relationship of piperine and its synthetic amide analogs for therapeutic potential to prevent experimentally induced ER stress in vitro.

Authors:  Ayat S Hammad; Sreenithya Ravindran; Ashraf Khalil; Shankar Munusamy
Journal:  Cell Stress Chaperones       Date:  2017-04-10       Impact factor: 3.667

Review 6.  Targeting the Holy Triangle of Quorum Sensing, Biofilm Formation, and Antibiotic Resistance in Pathogenic Bacteria.

Authors:  Ronit Vogt Sionov; Doron Steinberg
Journal:  Microorganisms       Date:  2022-06-16

7.  Chemosensitization of Trypanosoma congolense strains resistant to isometamidium chloride by tetracyclines and enrofloxacin.

Authors:  Vincent Delespaux; Hervé Sèna Vitouley; Tanguy Marcotty; Niko Speybroeck; Dirk Berkvens; Krisna Roy; Stanny Geerts; Peter Van den Bossche
Journal:  PLoS Negl Trop Dis       Date:  2010-09-28

8.  Bioenhancers from mother nature and their applicability in modern medicine.

Authors:  Gurpreet Kaur Randhawa; Jagdev Singh Kullar
Journal:  Int J Appl Basic Med Res       Date:  2011-01

9.  Bioenhancers: Revolutionary concept to market.

Authors:  Navin Atal; K L Bedi
Journal:  J Ayurveda Integr Med       Date:  2010-04

10.  Antimicrobial and efflux pump inhibitory activity of caffeoylquinic acids from Artemisia absinthium against gram-positive pathogenic bacteria.

Authors:  Yiannis C Fiamegos; Panagiotis L Kastritis; Vassiliki Exarchou; Haley Han; Alexandre M J J Bonvin; Jacques Vervoort; Kim Lewis; Michael R Hamblin; George P Tegos
Journal:  PLoS One       Date:  2011-04-04       Impact factor: 3.240

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