Carbonic anhydrase inhibitors. Inhibition of human erythrocyte isozymes I and II with a series of antioxidant phenols

SENTURK, Murat; Gülçin, İlhami; Daştan, Arif; Küfrevioğlu, Ömer İrfan; SUPURAN, Claudiu T.

doi:10.1016/j.bmc.2009.01.067

Makale Tam Makale Uluslararası 2009

Carbonic anhydrase inhibitors. Inhibition of human erythrocyte isozymes I and II with a series of antioxidant phenols

Murat SENTURK, İlhami Gülçin, Arif Daştan, Ömer İrfan Küfrevioğlu, Claudiu T. SUPURAN

BIOORGANIC & MEDICINAL CHEMISTRY Cilt 17 · Sayı 8 · ss. 3207–3211 · 15.04.2009

DOI ile aç

Özet

The inhibition of two human cytosolic carbonic anhydrase (hCA, EC 4.2.1.1) isozymes I and II, with a series of phenol derivatives was investigated by using the esterase assay, with 4- nitrophenyl acetate as substrate. 2,6-Dimethylphenol, 2,6-diisopropylphenol ( propofol), 2,6-di-t-butylphenol, butylated hydroxytoluene, butylated hydroxyanisole, vanillin, guaiacol, di(2,6-dimethylphenol), di( 2,6-diisopropylphenol), di( 2,6-di- t-butylphenol), and acetazolamide showed K-I values in the range of 37.5-274.5 mu M for hCA I and of 0.29 - 113.5 mu M against hCA II, respectively. All these phenols were non-competitive inhibitors with 4- nitrophenylacetate as substrate. Some antioxidant phenol derivatives investigated here showed effective hCA II inhibitory effects, in the same range as the clinically used sulfonamide acetazolamide, and might be used as leads for generating enzyme inhibitors possibly targeting other CA isoforms which have not been yet assayed for their interactions with such agents. (C) 2009 Elsevier Ltd. All rights reserved.

Anahtar kelimeler

carbonic anhydrase DERIVATIVES THERAPEUTIC APPLICATIONS BINDING HCA I Enzyme inhibitor SULFONAMIDES phenol hCA II RADICAL SCAVENGING ACTIVITIES 4 SALICYLIC-ACID METAL-COMPLEXES THIOXOLONE TARGETS VITRO ANTIOXIDANT 4 '-Biphenyl-1 1 '-diphenol

Atıf için künye

SENTURK, M., Gülçin, İ., Daştan, A., Küfrevioğlu, Ö. İ., & SUPURAN, C. T. (2009). Carbonic anhydrase inhibitors. Inhibition of human erythrocyte isozymes I and II with a series of antioxidant phenols. BIOORGANIC & MEDICINAL CHEMISTRY, 17(8), 3207–3211. https://doi.org/10.1016/j.bmc.2009.01.067

BibTeX

@article{senturk2009-67823,
  author = {SENTURK, Murat and Gülçin, İlhami and Daştan, Arif and Küfrevioğlu, Ömer İrfan and SUPURAN, Claudiu T.},
  title = {Carbonic anhydrase inhibitors. Inhibition of human erythrocyte isozymes I and II with a series of antioxidant phenols},
  journal = {BIOORGANIC & MEDICINAL CHEMISTRY},
  year = {2009},
  volume = {17},
  number = {8},
  pages = {3207--3211},
  issn = {0968-0896},
  doi = {10.1016/j.bmc.2009.01.067},
  url = {https://akademik.atauni.edu.tr/yayinlar/67823-carbonic-anhydrase-inhibitors-inhibition-of-human-erythrocyte-isozymes-i-and-ii}
}