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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...
Autores principales: | , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2019
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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. |
format | Online Article Text |
id | pubmed-6480344 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2019 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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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