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1,2,4-Oxadiazole/2-Imidazoline Hybrids: Multi-target-directed Compounds for the Treatment of Infectious Diseases and Cancer

Replacement of amide moiety with the 1,2,4-oxadiazole core in the scaffold of recently reported efflux pump inhibitors afforded a novel series of oxadiazole/2-imidazoline hybrids. The latter compounds exhibited promising antibacterial activity on both Gram-positive (Staphylococcus aureus, Bacillus s...

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Autores principales: Shetnev, Anton, Baykov, Sergey, Kalinin, Stanislav, Belova, Alexandra, Sharoyko, Vladimir, Rozhkov, Anton, Zelenkov, Lev, Tarasenko, Marina, Sadykov, Evgeny, Korsakov, Mikhail, Krasavin, Mikhail
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6480344/
https://www.ncbi.nlm.nih.gov/pubmed/30959765
http://dx.doi.org/10.3390/ijms20071699
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author Shetnev, Anton
Baykov, Sergey
Kalinin, Stanislav
Belova, Alexandra
Sharoyko, Vladimir
Rozhkov, Anton
Zelenkov, Lev
Tarasenko, Marina
Sadykov, Evgeny
Korsakov, Mikhail
Krasavin, Mikhail
author_facet Shetnev, Anton
Baykov, Sergey
Kalinin, Stanislav
Belova, Alexandra
Sharoyko, Vladimir
Rozhkov, Anton
Zelenkov, Lev
Tarasenko, Marina
Sadykov, Evgeny
Korsakov, Mikhail
Krasavin, Mikhail
author_sort Shetnev, Anton
collection PubMed
description Replacement of amide moiety with the 1,2,4-oxadiazole core in the scaffold of recently reported efflux pump inhibitors afforded a novel series of oxadiazole/2-imidazoline hybrids. The latter compounds exhibited promising antibacterial activity on both Gram-positive (Staphylococcus aureus, Bacillus subtilis) and Gram-negative (Escherichia coli, Pseudomonas fluorescens) strains. Furthermore, selected compounds markedly inhibited the growth of certain drug-resistant bacteria. Additionally, the study revealed the antiproliferative activity of several antibacterial frontrunners against pancreas ductal adenocarcinoma (PANC-1) cell line, as well as their type-selective monoamine oxidase (MAO) inhibitory profile.
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spelling pubmed-64803442019-04-29 1,2,4-Oxadiazole/2-Imidazoline Hybrids: Multi-target-directed Compounds for the Treatment of Infectious Diseases and Cancer Shetnev, Anton Baykov, Sergey Kalinin, Stanislav Belova, Alexandra Sharoyko, Vladimir Rozhkov, Anton Zelenkov, Lev Tarasenko, Marina Sadykov, Evgeny Korsakov, Mikhail Krasavin, Mikhail Int J Mol Sci Communication Replacement of amide moiety with the 1,2,4-oxadiazole core in the scaffold of recently reported efflux pump inhibitors afforded a novel series of oxadiazole/2-imidazoline hybrids. The latter compounds exhibited promising antibacterial activity on both Gram-positive (Staphylococcus aureus, Bacillus subtilis) and Gram-negative (Escherichia coli, Pseudomonas fluorescens) strains. Furthermore, selected compounds markedly inhibited the growth of certain drug-resistant bacteria. Additionally, the study revealed the antiproliferative activity of several antibacterial frontrunners against pancreas ductal adenocarcinoma (PANC-1) cell line, as well as their type-selective monoamine oxidase (MAO) inhibitory profile. MDPI 2019-04-05 /pmc/articles/PMC6480344/ /pubmed/30959765 http://dx.doi.org/10.3390/ijms20071699 Text en © 2019 by the authors. 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 (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Communication
Shetnev, Anton
Baykov, Sergey
Kalinin, Stanislav
Belova, Alexandra
Sharoyko, Vladimir
Rozhkov, Anton
Zelenkov, Lev
Tarasenko, Marina
Sadykov, Evgeny
Korsakov, Mikhail
Krasavin, Mikhail
1,2,4-Oxadiazole/2-Imidazoline Hybrids: Multi-target-directed Compounds for the Treatment of Infectious Diseases and Cancer
title 1,2,4-Oxadiazole/2-Imidazoline Hybrids: Multi-target-directed Compounds for the Treatment of Infectious Diseases and Cancer
title_full 1,2,4-Oxadiazole/2-Imidazoline Hybrids: Multi-target-directed Compounds for the Treatment of Infectious Diseases and Cancer
title_fullStr 1,2,4-Oxadiazole/2-Imidazoline Hybrids: Multi-target-directed Compounds for the Treatment of Infectious Diseases and Cancer
title_full_unstemmed 1,2,4-Oxadiazole/2-Imidazoline Hybrids: Multi-target-directed Compounds for the Treatment of Infectious Diseases and Cancer
title_short 1,2,4-Oxadiazole/2-Imidazoline Hybrids: Multi-target-directed Compounds for the Treatment of Infectious Diseases and Cancer
title_sort 1,2,4-oxadiazole/2-imidazoline hybrids: multi-target-directed compounds for the treatment of infectious diseases and cancer
topic Communication
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6480344/
https://www.ncbi.nlm.nih.gov/pubmed/30959765
http://dx.doi.org/10.3390/ijms20071699
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