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

Anton Shetnev, S. Baykov, Stanislav Kalinin, Alexandra Belova, Vladimir Sharoyko, Anton Rozhkov, Lev Zelenkov, Marina Tarasenko, Evgeny Sadykov, Mikhail Korsakov, Mikhail Krasavin

Research output

2 Citations (Scopus)

Abstract

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, Pseudomonasfluorescens) 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.

Original languageEnglish
Article number1699
Pages (from-to)1699
Number of pages10
JournalInternational Journal of Molecular Sciences
Volume20
Issue number7
DOIs
Publication statusPublished - 1 Apr 2019

Fingerprint

Oxadiazoles
infectious diseases
Bacilli
Amides
Scaffolds
Escherichia coli
Communicable Diseases
Bacteria
cancer
Cells
Pumps
efflux
pancreas
staphylococcus
Bacillus
oxidase
Monoamine Oxidase
Escherichia
Bacillus subtilis
cultured cells

Scopus subject areas

  • Molecular Biology
  • Spectroscopy
  • Catalysis
  • Inorganic Chemistry
  • Computer Science Applications
  • Physical and Theoretical Chemistry
  • Organic Chemistry

Cite this

@article{9949b7626c8f4ed990c896f897096492,
title = "1,2,4-Oxadiazole/2-Imidazoline Hybrids: Multi-target-directed Compounds for the Treatment of Infectious Diseases and Cancer",
abstract = "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, Pseudomonasfluorescens) 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.",
keywords = "1,2,4-oxadiazole, 2-imidazolines, Antibacterial, Cytotoxicity, MAO inhibition, DESIGN, VIVO, PERIPHERY, FURAZOLIDONE, OXADIAZOLE CLASS, antibacterial, IDENTIFICATION, DISCOVERY, IN-VITRO, 1,2, 4-oxadiazole, EXPLORATION, INHIBITORS, cytotoxicity",
author = "Anton Shetnev and S. Baykov and Stanislav Kalinin and Alexandra Belova and Vladimir Sharoyko and Anton Rozhkov and Lev Zelenkov and Marina Tarasenko and Evgeny Sadykov and Mikhail Korsakov and Mikhail Krasavin",
year = "2019",
month = "4",
day = "1",
doi = "10.3390/ijms20071699",
language = "English",
volume = "20",
pages = "1699",
journal = "International Journal of Molecular Sciences",
issn = "1422-0067",
publisher = "MDPI AG",
number = "7",

}

TY - JOUR

T1 - 1,2,4-Oxadiazole/2-Imidazoline Hybrids

T2 - Multi-target-directed Compounds for the Treatment of Infectious Diseases and Cancer

AU - Shetnev, Anton

AU - Baykov, S.

AU - Kalinin, Stanislav

AU - Belova, Alexandra

AU - Sharoyko, Vladimir

AU - Rozhkov, Anton

AU - Zelenkov, Lev

AU - Tarasenko, Marina

AU - Sadykov, Evgeny

AU - Korsakov, Mikhail

AU - Krasavin, Mikhail

PY - 2019/4/1

Y1 - 2019/4/1

N2 - 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, Pseudomonasfluorescens) 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.

AB - 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, Pseudomonasfluorescens) 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.

KW - 1,2,4-oxadiazole

KW - 2-imidazolines

KW - Antibacterial

KW - Cytotoxicity

KW - MAO inhibition

KW - DESIGN

KW - VIVO

KW - PERIPHERY

KW - FURAZOLIDONE

KW - OXADIAZOLE CLASS

KW - antibacterial

KW - IDENTIFICATION

KW - DISCOVERY

KW - IN-VITRO

KW - 1,2, 4-oxadiazole

KW - EXPLORATION

KW - INHIBITORS

KW - cytotoxicity

UR - http://www.scopus.com/inward/record.url?scp=85064550277&partnerID=8YFLogxK

UR - http://www.mendeley.com/research/124oxadiazole2imidazoline-hybrids-multitargetdirected-compounds-treatment-infectious-diseases-cancer

U2 - 10.3390/ijms20071699

DO - 10.3390/ijms20071699

M3 - Article

C2 - 30959765

VL - 20

SP - 1699

JO - International Journal of Molecular Sciences

JF - International Journal of Molecular Sciences

SN - 1422-0067

IS - 7

M1 - 1699

ER -