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Microbial Efflux Pump Inhibitors: A Journey around Quinoline and Indole Derivatives
Antimicrobial resistance (AMR) is a complex threat to human health and, to date, it represents a hot topic in drug discovery. The use of non-antibiotic molecules to block resistance mechanisms is a powerful alternative to the identification of new antibiotics. Bacterial efflux pumps exert the early...
Autores principales: | , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8618814/ https://www.ncbi.nlm.nih.gov/pubmed/34834098 http://dx.doi.org/10.3390/molecules26226996 |
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author | Cernicchi, Giada Felicetti, Tommaso Sabatini, Stefano |
author_facet | Cernicchi, Giada Felicetti, Tommaso Sabatini, Stefano |
author_sort | Cernicchi, Giada |
collection | PubMed |
description | Antimicrobial resistance (AMR) is a complex threat to human health and, to date, it represents a hot topic in drug discovery. The use of non-antibiotic molecules to block resistance mechanisms is a powerful alternative to the identification of new antibiotics. Bacterial efflux pumps exert the early step of AMR development, allowing the bacteria to grow in presence of sub-inhibitory drug concentration and develop more specific resistance mechanisms. Thus, efflux pump inhibitors (EPIs) offer a great opportunity to fight AMR, potentially restoring antibiotic activity. Based on our experience in designing and synthesizing novel EPIs, herein, we retrieved information around quinoline and indole derivatives reported in literature on this topic. Thus, our aim was to collect all data around these promising classes of EPIs in order to delineate a comprehensive structure–activity relationship (SAR) around each core for different microbes. With this review article, we aim to help future research in the field in the discovery of new microbial EPIs with improved activity and a better safety profile. |
format | Online Article Text |
id | pubmed-8618814 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-86188142021-11-27 Microbial Efflux Pump Inhibitors: A Journey around Quinoline and Indole Derivatives Cernicchi, Giada Felicetti, Tommaso Sabatini, Stefano Molecules Review Antimicrobial resistance (AMR) is a complex threat to human health and, to date, it represents a hot topic in drug discovery. The use of non-antibiotic molecules to block resistance mechanisms is a powerful alternative to the identification of new antibiotics. Bacterial efflux pumps exert the early step of AMR development, allowing the bacteria to grow in presence of sub-inhibitory drug concentration and develop more specific resistance mechanisms. Thus, efflux pump inhibitors (EPIs) offer a great opportunity to fight AMR, potentially restoring antibiotic activity. Based on our experience in designing and synthesizing novel EPIs, herein, we retrieved information around quinoline and indole derivatives reported in literature on this topic. Thus, our aim was to collect all data around these promising classes of EPIs in order to delineate a comprehensive structure–activity relationship (SAR) around each core for different microbes. With this review article, we aim to help future research in the field in the discovery of new microbial EPIs with improved activity and a better safety profile. MDPI 2021-11-19 /pmc/articles/PMC8618814/ /pubmed/34834098 http://dx.doi.org/10.3390/molecules26226996 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Review Cernicchi, Giada Felicetti, Tommaso Sabatini, Stefano Microbial Efflux Pump Inhibitors: A Journey around Quinoline and Indole Derivatives |
title | Microbial Efflux Pump Inhibitors: A Journey around Quinoline and Indole Derivatives |
title_full | Microbial Efflux Pump Inhibitors: A Journey around Quinoline and Indole Derivatives |
title_fullStr | Microbial Efflux Pump Inhibitors: A Journey around Quinoline and Indole Derivatives |
title_full_unstemmed | Microbial Efflux Pump Inhibitors: A Journey around Quinoline and Indole Derivatives |
title_short | Microbial Efflux Pump Inhibitors: A Journey around Quinoline and Indole Derivatives |
title_sort | microbial efflux pump inhibitors: a journey around quinoline and indole derivatives |
topic | Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8618814/ https://www.ncbi.nlm.nih.gov/pubmed/34834098 http://dx.doi.org/10.3390/molecules26226996 |
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