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Makale Tam Makale Uluslararası 2017

Synthesis of new cyclic thioureas and evaluation of their metal-chelating activity, acetylcholinesterase, butyrylcholinesterase, and carbonic anhydrase inhibition profiles

Parham TASLIMI, Afsun SUJAYEV, Emin Garibov, Nazar Nazarov, Zübeyir Huyut, Saleh H. ALWASEL, İlhami Gülçin

JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY Cilt 31 · Sayı 7 · 01.07.2017
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Özet

In the presence of trifluoracetic acid (TFAA), an efficient method for the synthesis of tetra(hexa)hydropyrimidinethione-carboxylates has been used on the basis of three-component condensation of thiourea with its different aldehydes and -diketones. Some novel cyclic thioureas were synthesized, and their hCA I, hCA II, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) inhibitors and metal-chelating properties were evaluated. K-i values of novel synthesized compounds for AChE and BChE are in the range of 51.84-135.96 and 143.96-274.55 nM, respectively. Also, HCA I and II were effectively inhibited by these novel compounds, with K-i values in the range of 404.16-745.13 nM for hCA I and of 434.20-689.57 nM for hCA II, respectively. Additionally, acetazolamide (AZA), clinically used as a CA inhibitor, with a K-i value of 883.68 +/- 121.27 nM in hCA I and 1008.66 +/- 144.70 nM in hCA II. Also, tacrine inhibited AChE and BChE showed K-i values of 314.63 +/- 31.66 and 373.57 +/- 75.07 nM, respectively.

Anahtar kelimeler

ANTIOXIDANT ACTIVITY carbonic anhydrase DERIVATIVES Acetylcholinesterase Butyrylcholinesterase ERYTHROCYTES IN-VITRO ENZYME-ACTIVITY PURIFICATION Thiourea POLYPHENOL CONTENTS LYOPHILIZED AQUEOUS EXTRACT Lactoperoxidase Avermectins ISOENZYMES HCA I Metal chelating

Atıf için künye

TASLIMI, P., SUJAYEV, A., Garibov, E., Nazarov, N., Huyut, Z., ALWASEL, S. H., & Gülçin, İ. (2017). Synthesis of new cyclic thioureas and evaluation of their metal-chelating activity, acetylcholinesterase, butyrylcholinesterase, and carbonic anhydrase inhibition profiles. JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY, 31(7). https://doi.org/10.1002/jbt.21897

BibTeX 
@article{taslimi2017-67674,
  author = {TASLIMI, Parham and SUJAYEV, Afsun and Garibov, Emin and Nazarov, Nazar and Huyut, Zübeyir and ALWASEL, Saleh H. and Gülçin, İlhami},
  title = {Synthesis of new cyclic thioureas and evaluation of their metal-chelating activity, acetylcholinesterase, butyrylcholinesterase, and carbonic anhydrase inhibition profiles},
  journal = {JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY},
  year = {2017},
  volume = {31},
  number = {7},
  issn = {1095-6670},
  doi = {10.1002/jbt.21897},
  url = {https://akademik.atauni.edu.tr/yayinlar/67674-synthesis-of-new-cyclic-thioureas-and-evaluation-of-their-metal-chelating}
}