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- Title
1,2,4-Oxadiazole/2-Imidazoline Hybrids: Multi-target-directed Compounds for the Treatment of Infectious Diseases and Cancer.
- Authors
Shetnev, Anton; Belova, Alexandra; Korsakov, Mikhail; Baykov, Sergey; Kalinin, Stanislav; Sharoyko, Vladimir; Rozhkov, Anton; Zelenkov, Lev; Krasavin, Mikhail; Tarasenko, Marina; Sadykov, Evgeny
- 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.
- Subjects
MONOAMINE oxidase; OXADIAZOLES; CANCER treatment; DRUG resistance in bacteria; PORINS (Proteins); NOVOBIOCIN; IMIDAZOLINES
- Publication
International Journal of Molecular Sciences, 2019, Vol 20, Issue 7, p1699
- ISSN
1661-6596
- Publication type
Article
- DOI
10.3390/ijms20071699