Novel carvacrol based new oxypropanolamine derivatives: Design, synthesis, characterization, biological evaluation, and molecular docking studies
Özet
Carvacrol, as a natural product used for many years in the treatment of various diseases, therefore it was chosen as the starting compound for this study. Novel carvacrol based new oxypropanolamine derivatives were synthesized and characterized by spectroscopic methods. All new compounds were tested as metabolic enzyme inhibitory agents. Their clinical usage of carvacrol has been established as diuretics, antiepileptics, and anti-glaucoma factors, in the management of gastric, duodenal ulcers, mountain sickness, osteoporosis, idiopathic intracranial hypertension, or neurological disorders. The in vitro anti-hyperglycemic screening results showed that the compound 3d exhibits the maximum inhibitory effect against alpha-glycosidase enzyme (IC50: 904.10 nM). In addition, the compounds 3d (IC50: 29.74 nM and 23.64 nM) and 3e (IC50: 31.28 nM and 26.11 nM) were found to have a significant response to inhibit carbonic anhydrase I, and II isoenzymes (hCA I and II), respectively. The novel carvacrol based oxypropanolamine compounds were effective inhibitors of the hCA I and II isozymes, and acetylcholinesterase with Ki values in the range of 27.18-44.84 nM for hCA I, 25.62-38.71 nM for hCA II, and 99.83-146.25 nM for AChE, respectively. (C) 2019 Elsevier B.V. All rights reserved.y
Anahtar kelimeler
Sürdürülebilir Kalkınma Amaçları
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SKA 15: Karasal Yaşam
Atıf için künye
Bytyqi-Damoni, A., Kestane, A., Taslimi, P., TÜZÜN, B., Zengin, M., Bilgicli, H. G., & Gülçin, İ. (2020). Novel carvacrol based new oxypropanolamine derivatives: Design, synthesis, characterization, biological evaluation, and molecular docking studies. Journal of Molecular Structure, 1202. https://doi.org/10.1016/j.molstruc.2019.127297
BibTeX
@article{bytyqidamoni2020-67871,
author = {Bytyqi-Damoni, Arlinda and Kestane, Ali and Taslimi, Parham and TÜZÜN, BURAK and Zengin, Mustafa and Bilgicli, Hayriye Genc and Gülçin, İlhami},
title = {Novel carvacrol based new oxypropanolamine derivatives: Design, synthesis, characterization, biological evaluation, and molecular docking studies},
journal = {Journal of Molecular Structure},
year = {2020},
volume = {1202},
issn = {0022-2860},
doi = {10.1016/j.molstruc.2019.127297},
url = {https://akademik.atauni.edu.tr/yayinlar/67871-novel-carvacrol-based-new-oxypropanolamine-derivatives-design-synthesis}
}