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Makale Tam Makale Ulusal 2020

Acetylcholinesterase inhibitory potency of new pyrazoline derivative

MEHTAP TUĞRAK, Halise İnci Gül, İlhami Gülçin

Journal of Research in Pharmacy Cilt 24 · Sayı 4 · ss. 464–471 · 01.01.2020
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Özet

Alzheimer's disease (AD) has no current cure and its mechanism is not fully known, but treatments for symptoms are available. Acetylcholinesterase (AChE) has been reported to be an applicable therapeutic target in patient with AD. Acetylcholinesterase inhibitors (AChEIs) are commonly used for it. For this purpose, novel series of pyrazoline based compounds [2-(3-(4-methoxypheny0-5-aryl-4,5-dihydro-1H-pyrazol-1-yl)benzo[d]thiazole,1-9] were synthesized and AChE inhibitory potencies were reported here. The results indicated that compound 1 (Ki= 0.13 +/- 0.004 mu M) possessed the highest AChE inhibitory effect in series, which is two times more potent than the reference compound Tacrin (Ki= 0.26 +/- 0.045 mu M). So, pyrazoline derivative 1 can be considered as a lead inhibitor in designing new AChE inhibitors.

Anahtar kelimeler

DISEASE Acetylcholinesterase Molecular docking BIOLOGICAL EVALUATION Pyrazoline CHALCONES ANTIFUNGAL ACTIVITY alzheimer disease benzothiazol SELECTIVE MONOAMINE-OXIDASE B INHIBITORS 3D-QSAR

Atıf için künye

TUĞRAK, M., Gül, H. İ., & Gülçin, İ. (2020). Acetylcholinesterase inhibitory potency of new pyrazoline derivative. Journal of Research in Pharmacy, 24(4), 464–471. https://doi.org/10.35333/jrp.2020.194

BibTeX
@article{tugrak2020-19955,
  author = {TUĞRAK, MEHTAP and Gül, Halise İnci and Gülçin, İlhami},
  title = {Acetylcholinesterase inhibitory potency of new pyrazoline derivative},
  journal = {Journal of Research in Pharmacy},
  year = {2020},
  volume = {24},
  number = {4},
  pages = {464--471},
  issn = {2630-6344},
  doi = {10.35333/jrp.2020.194},
  url = {https://akademik.atauni.edu.tr/yayinlar/19955-acetylcholinesterase-inhibitory-potency-of-new-pyrazoline-derivative}
}