Literature DB >> 27977195

Improved Potency of Indole-Based NorA Efflux Pump Inhibitors: From Serendipity toward Rational Design and Development.

Federica Buonerba1, Susan Lepri1, Laura Goracci1, Bryan D Schindler2, Susan M Seo2, Glenn W Kaatz2,3, Gabriele Cruciani1.   

Abstract

The NorA efflux pump is a potential drug target for reversal of resistance to selected antibacterial agents, and recently we described indole-based inhibitor candidates. Herein we report a second class of inhibitors derived from them but with significant differences in shape and size. In particular, compounds 13 and 14 are very potent inhibitors in that they demonstrated the lowest IC50 values (2 μM) ever observed among all indole-based compounds we have evaluated.

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Year:  2016        PMID: 27977195     DOI: 10.1021/acs.jmedchem.6b01281

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  8 in total

1.  Clinically Approved Drugs Inhibit the Staphylococcus aureus Multidrug NorA Efflux Pump and Reduce Biofilm Formation.

Authors:  Saskia Zimmermann; Mareike Klinger-Strobel; Jürgen A Bohnert; Sindy Wendler; Jürgen Rödel; Mathias W Pletz; Bettina Löffler; Lorena Tuchscherr
Journal:  Front Microbiol       Date:  2019-12-03       Impact factor: 5.640

Review 2.  Microbial Efflux Pump Inhibitors: A Journey around Quinoline and Indole Derivatives.

Authors:  Giada Cernicchi; Tommaso Felicetti; Stefano Sabatini
Journal:  Molecules       Date:  2021-11-19       Impact factor: 4.411

Review 3.  Relationships between Efflux Pumps and Emergence of Heteroresistance: A Comprehensive Study on the Current Findings.

Authors:  Mohammad Abavisani; Mansoor Kodori; Fariba Akrami; Ali Radfar; Ali Hashemi
Journal:  Can J Infect Dis Med Microbiol       Date:  2022-09-19       Impact factor: 2.585

4.  Effect of Carvacrol and Thymol on NorA efflux pump inhibition in multidrug-resistant (MDR) Staphylococcus aureus strains.

Authors:  Cristina Rodrigues Dos Santos Barbosa; Jackelyne Roberta Scherf; Thiago Sampaio de Freitas; Irwin Rose Alencar de Menezes; Raimundo Luiz Silva Pereira; Joycy Francely Sampaio Dos Santos; Sarah Silva Patrício de Jesus; Thais Pereira Lopes; Zildene de Sousa Silveira; Cícera Datiane de Morais Oliveira-Tintino; José Pinto Siqueira Júnior; Henrique Douglas Melo Coutinho; Saulo Relison Tintino; Francisco Assis Bezerra da Cunha
Journal:  J Bioenerg Biomembr       Date:  2021-06-22       Impact factor: 2.945

5.  Microbe-Derived Indole Metabolite Demonstrates Potent Multidrug Efflux Pump Inhibition in Staphylococcus aureus.

Authors:  Rushikesh Tambat; Manoj Jangra; Nisha Mahey; Nishtha Chandal; Manpreet Kaur; Surbhi Chaudhary; Dipesh Kumar Verma; Krishan Gopal Thakur; Manoj Raje; Sanjay Jachak; Neeraj Khatri; Hemraj Nandanwar
Journal:  Front Microbiol       Date:  2019-09-18       Impact factor: 5.640

6.  Structural Modifications of the Quinolin-4-yloxy Core to Obtain New Staphylococcus aureus NorA Inhibitors.

Authors:  Rolando Cannalire; Gianmarco Mangiaterra; Tommaso Felicetti; Andrea Astolfi; Nicholas Cedraro; Serena Massari; Giuseppe Manfroni; Oriana Tabarrini; Salvatore Vaiasicca; Maria Letizia Barreca; Violetta Cecchetti; Francesca Biavasco; Stefano Sabatini
Journal:  Int J Mol Sci       Date:  2020-09-24       Impact factor: 5.923

7.  From Quinoline to Quinazoline-Based S. aureus NorA Efflux Pump Inhibitors by Coupling a Focused Scaffold Hopping Approach and a Pharmacophore Search.

Authors:  Nicholas Cedraro; Rolando Cannalire; Andrea Astolfi; Gianmarco Mangiaterra; Tommaso Felicetti; Salvatore Vaiasicca; Giada Cernicchi; Serena Massari; Giuseppe Manfroni; Oriana Tabarrini; Violetta Cecchetti; Maria Letizia Barreca; Francesca Biavasco; Stefano Sabatini
Journal:  ChemMedChem       Date:  2021-06-26       Impact factor: 3.466

Review 8.  Efflux Pump Mediated Antimicrobial Resistance by Staphylococci in Health-Related Environments: Challenges and the Quest for Inhibition.

Authors:  Abolfazl Dashtbani-Roozbehani; Melissa H Brown
Journal:  Antibiotics (Basel)       Date:  2021-12-07
  8 in total

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