Synthesis of 4,5-disubstituted-2-thioxo-1,2,3,4-tetrahydropyrimidines and investigation of their acetylcholinesterase, butyrylcholinesterase, carbonic anhydrase I/II inhibitory and antioxidant activities

Garibov, Emin; TASLIMI, Parham; SUJAYEV, Afsun; BINGOL, Zeynebe; CETINKAYA, Songul; Gülçin, İlhami; Beydemir, Sukru; FARZALIYEV, Vagif; ALWASEL, Saleh H.; SUPURAN, Claudiu T.

doi:10.1080/14756366.2016.1198901

Makale Tam Makale Uluslararası 2016

Synthesis of 4,5-disubstituted-2-thioxo-1,2,3,4-tetrahydropyrimidines and investigation of their acetylcholinesterase, butyrylcholinesterase, carbonic anhydrase I/II inhibitory and antioxidant activities

Emin Garibov, Parham TASLIMI, Afsun SUJAYEV, Zeynebe BINGOL, Songul CETINKAYA, İlhami Gülçin, Sukru Beydemir, Vagif FARZALIYEV, Saleh H. ALWASEL, Claudiu T. SUPURAN

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY Cilt 31 · ss. 1–9 · 01.12.2016

DOI ile aç

Özet

A series of tetrahydropyrimidinethiones were synthesized from thiourea, -diketones and aromatic aldehydes, such as p-tolualdehyde, p-anisaldehyde, o-tolualdehyde, salicylaldehyde and benzaldehyde. These cyclic thioureas showed good inhibitory action against acetylcholine esterase (AChE), butyrylcholine esterase (BChE), and human (h) carbonic anhydrase (CA) isoforms I and II. AChE and BChE inhibitions were in the range of 6.11-16.13 and 6.76-15.68nM, respectively. hCA I and II were effectively inhibited by these compounds, with K-i values in the range of 47.40-76.06nM for hCA I, and of 30.63-76.06nM for hCA II, respectively. The antioxidant activity of the cyclic thioureas was investigated by using different in vitro antioxidant assays, including 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging, Cu(2+)and Fe(3+)reducing, and Fe(2+)chelating activities.

Anahtar kelimeler

ANTIOXIDANT ACTIVITY carbonic anhydrase L. Acetylcholinesterase Butyrylcholinesterase enzyme inhibition SULFONAMIDE DERIVATIVES ERYTHROCYTE ISOZYMES I IN-VITRO ANTIOXIDANT POLYPHENOL CONTENTS LYOPHILIZED AQUEOUS EXTRACT RADICAL SCAVENGING ACTIVITY ANTIRADICAL ACTIVITIES ISOENZYMES HCA I ESTERASE

Atıf için künye

Garibov, E., TASLIMI, P., SUJAYEV, A., BINGOL, Z., CETINKAYA, S., Gülçin, İ., Beydemir, S., FARZALIYEV, V., ALWASEL, S. H., & SUPURAN, C. T. (2016). Synthesis of 4,5-disubstituted-2-thioxo-1,2,3,4-tetrahydropyrimidines and investigation of their acetylcholinesterase, butyrylcholinesterase, carbonic anhydrase I/II inhibitory and antioxidant activities. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 31, 1–9. https://doi.org/10.1080/14756366.2016.1198901

BibTeX

@article{garibov2016-67828,
  author = {Garibov, Emin and TASLIMI, Parham and SUJAYEV, Afsun and BINGOL, Zeynebe and CETINKAYA, Songul and Gülçin, İlhami and Beydemir, Sukru and FARZALIYEV, Vagif and ALWASEL, Saleh H. and SUPURAN, Claudiu T.},
  title = {Synthesis of 4,5-disubstituted-2-thioxo-1,2,3,4-tetrahydropyrimidines and investigation of their acetylcholinesterase, butyrylcholinesterase, carbonic anhydrase I/II inhibitory and antioxidant activities},
  journal = {JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY},
  year = {2016},
  volume = {31},
  pages = {1--9},
  issn = {1475-6366},
  doi = {10.1080/14756366.2016.1198901},
  url = {https://akademik.atauni.edu.tr/yayinlar/67828-synthesis-of-45-disubstituted-2-thioxo-1234-tetrahydropyrimidines-and}
}