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Makale Tam Makale Uluslararası 2018

Novel thymol bearing oxypropanolamine derivatives as potent some metabolic enzyme inhibitors - Their antidiabetic, anticholinergic and antibacterial potentials

Mustafa Zengin, Hayriye Genc, Parham TASLIMI, Ali Kestane, Ertugrul Guclu, Aziz Ogutlu, Oguz Karabay, İlhami Gülçin

Bioorganic Chemistry Cilt 81 · ss. 119–126 · 01.12.2018
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Özet

A series of classical and newly synthesized thymol bearing oxypropanolamine compounds were synthesized and characterized. Their in vitro antibacterial activity on A. baumannii, P. aeruginosa, E. coli and S. aureus strains were investigated with agar well diffusion method. The results were compared with commercially available drug active compounds. As well as 3a, 3b and 3c have the most significant antibacterial effect among all the tested compounds; approximately all of them have more antibacterial activity than the reference drugs. These novel thymol bearing oxypropanolamine derivatives were effective inhibitors of the a-glycosidase, cytosolic carbonic anhydrase I and II isoforms (hCA I and II), and acetylcholinesterase enzymes (AChE) with K-f values in the range of 463.85-851.05 mu M for alpha-glycosidase, 1.11-17.34 mu M for hCA I, 2.97-17.83 mu M for hCA II, and 13.58-31.45 mu M for AChE, respectively.

Anahtar kelimeler

ANTIMICROBIAL ACTIVITY carbonic anhydrase IN-VIVO Acetylcholinesterase Butyrylcholinesterase ESSENTIAL OIL Natural products Mannich bases alpha-glycosidase ALPHA-GLUCOSIDASE INHIBITORS Antibacterial effects II INHIBITION Oxypropanolamine

Atıf için künye

Zengin, M., Genc, H., TASLIMI, P., Kestane, A., Guclu, E., Ogutlu, A., Karabay, O., & Gülçin, İ. (2018). Novel thymol bearing oxypropanolamine derivatives as potent some metabolic enzyme inhibitors - Their antidiabetic, anticholinergic and antibacterial potentials. Bioorganic Chemistry, 81, 119–126. https://doi.org/10.1016/j.bioorg.2018.08.003

BibTeX
@article{zengin2018-68093,
  author = {Zengin, Mustafa and Genc, Hayriye and TASLIMI, Parham and Kestane, Ali and Guclu, Ertugrul and Ogutlu, Aziz and Karabay, Oguz and Gülçin, İlhami},
  title = {Novel thymol bearing oxypropanolamine derivatives as potent some metabolic enzyme inhibitors - Their antidiabetic, anticholinergic and antibacterial potentials},
  journal = {Bioorganic Chemistry},
  year = {2018},
  volume = {81},
  pages = {119--126},
  issn = {0045-2068},
  doi = {10.1016/j.bioorg.2018.08.003},
  url = {https://akademik.atauni.edu.tr/yayinlar/68093-novel-thymol-bearing-oxypropanolamine-derivatives-as-potent-some-metabolic}
}