In vitro inhibition of purified human carbonic anhydrase I and II by novel fluorene derivatives

Authors

  • Hülya Demirhan Sakarya University
  • Mustafa Arslan Sakarya University
  • Mustafa Oguzhan Kaya Balikesir University
  • Yeşim Kaya Balikesir Universtiy
  • Nahit Gençer Department of Chemistry, Faculty of Art and Sciences, Balikesir University
  • Oktay Arslan Balikesir University

DOI:

https://doi.org/10.20450/mjcce.2014.440

Keywords:

9-benzylidene-9H-fluorene, urea, thiourea, carbonic anhydrase, inhibition

Abstract

In this study, 9-benzylidene-9H-fluorene-substituted urea (5a–p) and thiourea derivatives (5q–v) were synthesized and their inhibitory effects on the activity of human carbonic anhydrase (hCA) I and II were evaluated. hCA I and II were purified from human erythrocytes using a Sepharose 4B-L-tyrosine-sulphanilamide affinity column. All the synthesized compounds inhibited the activity of the hCA I and II isoenzymes. Among the synthesized compounds, 5f was found to be the most active (IC50 = 21.4 μM) for inhibition of hCA I and 5s was the most active (IC50 = 25.3 μM) for inhibition of hCA II.


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Published

2014-09-15

How to Cite

Demirhan, H., Arslan, M., Kaya, M. O., Kaya, Y., Gençer, N., & Arslan, O. (2014). In vitro inhibition of purified human carbonic anhydrase I and II by novel fluorene derivatives. Macedonian Journal of Chemistry and Chemical Engineering, 33(2), 199–207. https://doi.org/10.20450/mjcce.2014.440

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Section

Biochemistry