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Makale Tam Makale Uluslararası 2016

Synthesis of 4-(2-substituted hydrazinyl)benzenesulfonamides and their carbonic anhydrase inhibitory effects

Halise İnci Gül, Kaan Kucukoglu, Cem Yamalı, Sinan Bilginer, Hafize Yuca, Iknur Ozturk, Parham Taslımı, İlhami Gülçin, Claudiu T. Supuran

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY Cilt 31 · ss. 568–573 · 01.01.2016
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Özet

In this study, 4-(2-substituted hydrazinyl)benzenesulfonamides were synthesized by microwave irradiation and their chemical structures were confirmed by H-1 NMR, (CNMR)-C-13, and HRMS. Ketones used were: Acetophenone (S1), 4-methylacetophenone (S2), 4-chloroacetophenone (S3), 4-fluoroacetophenone (S4), 4-bromoacetophenone (S5), 4-methoxyacetophenone (S6), 4-nitroacetophenone (S7), 2-acetylthiophene (S8), 2-acetylfuran (S9), 1-indanone (S10), 2-indanone (S11). The compounds S9, S10 and S11 were reported for the first time, while S1-S8 was synthesized by different method than literature reported using microwave irradiation method instead of conventional heating in this study. The inhibitory effects of 4-(2-substituted hydrazinyl) benzenesulfonamide derivatives (S1-S11) against hCA I and II were studied. Cytosolic hCA I and II isoenzymes were potently inhibited by new synthesized sulphonamide derivatives with K-is in the range of 1.79 +/- 0.22-2.73 +/- 0.08 nM against hCA I and in the range of 1.72 +/- 0.58-11.64 +/- 5.21nM against hCA II, respectively.

Anahtar kelimeler

carbonic anhydrase enzyme inhibition 2-Acethylfuran 2-acethylthiophene acetophenones indanone sulfonamide TROUT ONCORHYNCHUS-MYKISS ERYTHROCYTES IN-VITRO THERAPEUTIC APPLICATIONS SULFONAMIDE DERIVATIVES ENZYME-ACTIVITY ISOENZYMES I ISOZYMES I ISOFORMS I PURIFICATION PEROXIDASE

Atıf için künye

Gül, H. İ., Kucukoglu, K., Yamalı, C., Bilginer, S., Yuca, H., Ozturk, I., Taslımı, P., Gülçin, İ., & Supuran, C. T. (2016). Synthesis of 4-(2-substituted hydrazinyl)benzenesulfonamides and their carbonic anhydrase inhibitory effects. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 31, 568–573. https://doi.org/10.3109/14756366.2015.1047359

BibTeX 
@article{gul2016-18570,
  author = {Gül, Halise İnci and Kucukoglu, Kaan and Yamalı, Cem and Bilginer, Sinan and Yuca, Hafize and Ozturk, Iknur and Taslımı, Parham and Gülçin, İlhami and Supuran, Claudiu T.},
  title = {Synthesis of 4-(2-substituted hydrazinyl)benzenesulfonamides and their carbonic anhydrase inhibitory effects},
  journal = {JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY},
  year = {2016},
  volume = {31},
  pages = {568--573},
  issn = {1475-6366},
  doi = {10.3109/14756366.2015.1047359},
  url = {https://akademik.atauni.edu.tr/yayinlar/18570-synthesis-of-4-2-substituted-hydrazinylbenzenesulfonamides-and-their-carbonic}
}