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Inhibitory effects of isatin Mannich bases on carbonic anhydrases, acetylcholinesterase, and butyrylcholinesterase

Dilan Ozmen Ozgun, Cem Yamalı, Halise İnci Gül, Parham Taslımı, İlhami Gülçin, Telat Yanık, Claudiu T. Supuran

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY Cilt 31 · Sayı 6 · ss. 1498–1501 · 01.01.2016
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Özet

The effects of isatin Mannich bases incorporating (1-[piperidin-1-yl (P1)/morpholin-4-yl (P2)/N-methylpiperazin-1-yl (P3)]methyl)-1H-indole-2,3-dione) moieties against human (h) carbonic anhydrase (CA, EC 4.2.1.1) isoenzymes hCA I and hCA II, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) enzymes were evaluated. P1-P3 demonstrated impressive inhibition profiles against AChE and BChE and also inhibited both CAs at nanomolar level. These inhibitory effects were more powerful in all cases than the reference compounds used for all these enzymes. This study suggests that isatin Mannich bases P1-P3 are good candidate compounds especially for the development of new cholinesterase inhibitors since they were 2.2-5.9 times better inhibitors than clinically used drug Tacrine.

Anahtar kelimeler

carbonic anhydrase cytotoxicity DERIVATIVES Acetylcholinesterase Butyrylcholinesterase DISCOVERY BIOLOGICAL EVALUATION Mannich bases isatin DNA TOPOISOMERASE-I CORRESPONDING PIPERIDINOLS MEDICINAL CHEMISTRY JURKAT CELLS HYDROCHLORIDES DIHYDROCHLORIDE

Atıf için künye

Ozgun, D. O., Yamalı, C., Gül, H. İ., Taslımı, P., Gülçin, İ., Yanık, T., & Supuran, C. T. (2016). Inhibitory effects of isatin Mannich bases on carbonic anhydrases, acetylcholinesterase, and butyrylcholinesterase. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 31(6), 1498–1501. https://doi.org/10.3109/14756366.2016.1149479

BibTeX 
@article{ozgun2016-19852,
  author = {Ozgun, Dilan Ozmen and Yamalı, Cem and Gül, Halise İnci and Taslımı, Parham and Gülçin, İlhami and Yanık, Telat and Supuran, Claudiu T.},
  title = {Inhibitory effects of isatin Mannich bases on carbonic anhydrases, acetylcholinesterase, and butyrylcholinesterase},
  journal = {JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY},
  year = {2016},
  volume = {31},
  number = {6},
  pages = {1498--1501},
  issn = {1475-6366},
  doi = {10.3109/14756366.2016.1149479},
  url = {https://akademik.atauni.edu.tr/yayinlar/19852-inhibitory-effects-of-isatin-mannich-bases-on-carbonic-anhydrases}
}