1,2,4-Oxadiazole/2-Imidazoline Hybrids: Multi-target-directed Compounds for the Treatment of Infectious Diseases and Cancer.
Anton A ShetnevSergey BaykovStanislav KalininAlexandra BelovaVladimir SharoykoAnton V RozhkovLev E ZelenkovMarina TarasenkoEvgeny SadykovMikhail KorsakovMikhail KrasavinPublished in: International journal of molecular sciences (2019)
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.
Keyphrases
- gram negative
- multidrug resistant
- drug resistant
- escherichia coli
- infectious diseases
- acinetobacter baumannii
- bacillus subtilis
- klebsiella pneumoniae
- staphylococcus aureus
- biofilm formation
- papillary thyroid
- silver nanoparticles
- squamous cell carcinoma
- single cell
- squamous cell
- radiation therapy
- replacement therapy
- locally advanced