Novel eugenol bearing oxypropanolamines: Synthesis, characterization, antibacterial, antidiabetic, and anticholinergic potentials

Bilgicli H. G., Kestane A., Taslimi P., Karabay O., Bytyqi-Damoni A., Zengin M., ...Daha Fazla

BIOORGANIC CHEMISTRY, cilt.88, 2019 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 88
  • Basım Tarihi: 2019
  • Doi Numarası: 10.1016/j.bioorg.2019.102931
  • Dergi Adı: BIOORGANIC CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Anahtar Kelimeler: Eugenol, Antibacterial effects, alpha-glycosidase, Carbonic anhydrase, Acetylcholinesterase, Enzyme inhibition, ANHYDRASE INHIBITORY PROPERTIES, CARBONIC-ANHYDRASE, ACETYLCHOLINE ESTERASE, BIOLOGICAL EVALUATION, ALPHA-GLUCOSIDASE, CRYSTAL-STRUCTURE, ISOENZYMES I, BUTYRYLCHOLINESTERASE, DERIVATIVES, ANTIOXIDANT
  • Atatürk Üniversitesi Adresli: Evet

Özet

Five oxypropanol amine derivatives that four of them are novel have been synthesized with high yields and practical methods. in vitro antibacterial susceptibility of Acinetobacter baumannii, Pseudomonas aeruginosa, Escherichia coli and Staphylococcus aureus strains to synthesized substances were evaluated with agar well-diffusion method by comparison with commercially available drugs. Most of the bacteria were multidrug resistant. It was concluded that these compounds are much more effective than reference drugs. These eugenol bearing oxypropanolamine derivatives were also effective inhibitors against alpha-glycosidase, cytosolic carbonic anhydrase I and II isoforms (hCA I and II), and acetylcholinesterase (AChE) enzymes with K-i values in the range of 0.80 +/- 0.24-3.52 +/- 1.01 mu M for hCA I, 1.08 +/- 0.15-3.64 +/- 0.92 mu M for hCA II, 5.18 +/- 0.84-12.46 +/- 2.08 mu M for alpha-glycosidase, and 11.33 +/- 2.83-32.81 +/- 9.73 mu M for AChE, respectively.