2H-Indazolo[2,1-b]phthalazine-trione derivatives: Inhibition on some metabolic enzymes and molecular docking studies
Özet
In this study, substituted 2H-indazolo[2,1-b]phthalazine-1,6,11-trione compounds (4a-d) obtained via one-pot three-component condensation reaction of aromatic aldehydes, cyclic 1,3-dione, and phthalhydrazide in ethanol catalyzed by Y(OTf)(3) showed satisfactory inhibitory effects against some important enzymes. Also, these molecules had K-i values in the row of 185.92 +/- 36.03-294.82 +/- 50.76 nM vs carbonic anhydrase I (CA I), 204.93 +/- 46.90-374.10 +/- 83.63 nM against human CA II, 937.16 +/- 205.82-1021.83 +/- 193.66 nM against alpha-glycosidase (alpha-Gly), respectively. For cholinesterase enzymes, the K-i values were found in the range of 47.26 +/- 9.62-72.05 +/- 19.47 nM against acetylcholinesterase (AChE) and 65.03 +/- 9.88-102.83 +/- 25.04 nM against butyrylcholinesterase (BChE), respectively. The inhibition effects of these compounds against enzymes whose name are AChE, BChE, alpha-Gly, hCA I, and hCA II, were compared with control molecules like tacrine, acarbose, and acetazolamide.
Atıf için künye
Taslimi, P., Türkan, F., TURHAN, K., Karaman, H. S., TURGUT, Z., & Gülçin, İ. (2020). 2H-Indazolo[2,1-b]phthalazine-trione derivatives: Inhibition on some metabolic enzymes and molecular docking studies. Journal of Heterocyclic Chemistry, 57(8), 3116–3125. https://doi.org/10.1002/jhet.4019
BibTeX
@article{taslimi2020-67855,
author = {Taslimi, Parham and Türkan, Fikret and TURHAN, Kadir and Karaman, Halide Sedef and TURGUT, Zühal and Gülçin, İlhami},
title = {2H-Indazolo[2,1-b]phthalazine-trione derivatives: Inhibition on some metabolic enzymes and molecular docking studies},
journal = {Journal of Heterocyclic Chemistry},
year = {2020},
volume = {57},
number = {8},
pages = {3116--3125},
issn = {0022-152X},
doi = {10.1002/jhet.4019},
url = {https://akademik.atauni.edu.tr/yayinlar/67855-2h-indazolo21-bphthalazine-trione-derivatives-inhibition-on-some-metabolic}
}