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Makale Tam Makale Uluslararası 2018

Synthesis and investigation of the conversion reactions of pyrimidine-thiones with nucleophilic reagent and evaluation of their acetylcholinesterase, carbonic anhydrase inhibition, and antioxidant activities

Parham TASLIMI, Afsun Sujayev, Fikret Turkan, Emin Garibov, Zübeyir Huyut, Vagif Farzaliyev, Sevgi MAMEDOVA, İlhami Gülçin

JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY Cilt 32 · Sayı 2 · 01.02.2018
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Özet

The conversion reactions of pyrimidine-thiones with nucleophilic reagent were studied during this scientific research. For this purpose, new compounds were synthesized by the interaction between 1,2-epoxy propane, 1,2-epoxy butane, and 4-chlor-1-butanol and pyrimidine-thiones. These pyrimidine-thiones derivatives (A-K) showed good inhibitory action against acetylcholinesterase (AChE), and human carbonic anhydrase (hCA) isoforms I and II. AChE inhibition was in the range of 93.1 +/- 33.7-467.5 +/- 126.9nM. The hCA I and II were effectively inhibited by these compounds, with K-i values in the range of 4.3 +/- 1.1-9.1 +/- 2.7nM for hCA I and 4.2 +/- 1.1-14.1 +/- 4.4nM for hCA II. On the other hand, acetazolamide clinically used as CA inhibitor showed K-i value of 13.9 +/- 5.1nM against hCA I and 18.1 +/- 8.5nM against hCA II. The antioxidant activity of the pyrimidine-thiones derivatives (A-K) was investigated by using different in vitro antioxidant assays, including Cu(2+)and Fe(3+)reducing, 1,1-diphenyl-2-picrylhydrazyl (DPPH center dot) radical scavenging, and Fe(2+)chelating activities.

Anahtar kelimeler

ANTIOXIDANT ACTIVITY carbonic anhydrase Acetylcholinesterase enzyme inhibition ERYTHROCYTES IN-VITRO ENZYME-ACTIVITY ISOENZYMES I PHENETHYL ESTER CAPE CAFFEIC ACID ANALGESIC ACTIVITIES LYOPHILIZED AQUEOUS EXTRACT ANTIRADICAL ACTIVITIES CHIONANTHUS-VIRGINICUS L. STRUCTURE-ACTIVITY INSIGHT pyrimidine-thiones

Atıf için künye

TASLIMI, P., Sujayev, A., Turkan, F., Garibov, E., Huyut, Z., Farzaliyev, V., MAMEDOVA, S., & Gülçin, İ. (2018). Synthesis and investigation of the conversion reactions of pyrimidine-thiones with nucleophilic reagent and evaluation of their acetylcholinesterase, carbonic anhydrase inhibition, and antioxidant activities. JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY, 32(2). https://doi.org/10.1002/jbt.22019

BibTeX 
@article{taslimi2018-67995,
  author = {TASLIMI, Parham and Sujayev, Afsun and Turkan, Fikret and Garibov, Emin and Huyut, Zübeyir and Farzaliyev, Vagif and MAMEDOVA, Sevgi and Gülçin, İlhami},
  title = {Synthesis and investigation of the conversion reactions of pyrimidine-thiones with nucleophilic reagent and evaluation of their acetylcholinesterase, carbonic anhydrase inhibition, and antioxidant activities},
  journal = {JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY},
  year = {2018},
  volume = {32},
  number = {2},
  issn = {1095-6670},
  doi = {10.1002/jbt.22019},
  url = {https://akademik.atauni.edu.tr/yayinlar/67995-synthesis-and-investigation-of-the-conversion-reactions-of-pyrimidine-thiones}
}