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...

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Autores principales:	Giada Cernicchi, Tommaso Felicetti, Stefano Sabatini
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	efflux pump inhibitors antibiotic resistance breakers microbial efflux pumps antimicrobial resistance antibiotic resistance Organic chemistry QD241-441
Acceso en línea:	https://doaj.org/article/e79a2cf4b97140a097c7c5abf29c00a3
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spelling	oai:doaj.org-article:e79a2cf4b97140a097c7c5abf29c00a32021-11-25T18:29:07ZMicrobial Efflux Pump Inhibitors: A Journey around Quinoline and Indole Derivatives10.3390/molecules262269961420-3049https://doaj.org/article/e79a2cf4b97140a097c7c5abf29c00a32021-11-01T00:00:00Zhttps://www.mdpi.com/1420-3049/26/22/6996https://doaj.org/toc/1420-3049Antimicrobial 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.Giada CernicchiTommaso FelicettiStefano SabatiniMDPI AGarticleefflux pump inhibitorsantibiotic resistance breakersmicrobial efflux pumpsantimicrobial resistanceantibiotic resistanceOrganic chemistryQD241-441ENMolecules, Vol 26, Iss 6996, p 6996 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	efflux pump inhibitors antibiotic resistance breakers microbial efflux pumps antimicrobial resistance antibiotic resistance Organic chemistry QD241-441
spellingShingle	efflux pump inhibitors antibiotic resistance breakers microbial efflux pumps antimicrobial resistance antibiotic resistance Organic chemistry QD241-441 Giada Cernicchi Tommaso Felicetti Stefano Sabatini Microbial Efflux Pump Inhibitors: A Journey around Quinoline and Indole Derivatives
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	article
author	Giada Cernicchi Tommaso Felicetti Stefano Sabatini
author_facet	Giada Cernicchi Tommaso Felicetti Stefano Sabatini
author_sort	Giada Cernicchi
title	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_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_sort	microbial efflux pump inhibitors: a journey around quinoline and indole derivatives
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/e79a2cf4b97140a097c7c5abf29c00a3
work_keys_str_mv	AT giadacernicchi microbialeffluxpumpinhibitorsajourneyaroundquinolineandindolederivatives AT tommasofelicetti microbialeffluxpumpinhibitorsajourneyaroundquinolineandindolederivatives AT stefanosabatini microbialeffluxpumpinhibitorsajourneyaroundquinolineandindolederivatives
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Microbial Efflux Pump Inhibitors: A Journey around Quinoline and Indole Derivatives

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