scholarly journals Synthesis and In Vitro Inhibition Effect of New Pyrido[2,3-d]pyrimidine Derivatives on Erythrocyte Carbonic Anhydrase I and II

2014 ◽  
Vol 2014 ◽  
pp. 1-8 ◽  
Author(s):  
Hilal Kuday ◽  
Fatih Sonmez ◽  
Cigdem Bilen ◽  
Emre Yavuz ◽  
Nahit Gençer ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Inhibitory Activity ◽  
Pyrimidine Derivatives ◽  
Structure Activity ◽  
Carbonic Anhydrase I ◽  
Activity Structure ◽  
In Vitro Inhibition ◽  
Inhibitory Activities ◽  
Erythrocyte Carbonic Anhydrase

In vitro inhibition effects of indolylchalcones and new pyrido[2,3-d]pyrimidine derivatives on purified human carbonic anhydrase I and II (hCA I and II) were investigated by using CO2as a substrate. The results showed that all compounds inhibited the hCA I and hCA II enzyme activities. Among all the synthesized compounds,7e(IC50=6.79 µM) was found to be the most active compound for hCA I inhibitory activity and5g(IC50=7.22 µM) showed the highest hCA II inhibitory activity. Structure-activity relationships study showed that indolylchalcone derivatives have higher inhibitory activities than pyrido[2,3-d]pyrimidine derivatives on hCA I and hCA II. Additionally, methyl group bonded to uracil ring increases inhibitory activities on both hCA I and hCA II.

In vitro inhibition effect of some chalcones on erythrocyte carbonic anhydrase I and II

2013 ◽  
Vol 41 (6) ◽  
pp. 384-388 ◽  
Author(s):  
Nahit Gençer ◽  
Çiğdem Bilen ◽  
Dudu Demir ◽  
Alparslan Atahan ◽  
Mustafa Ceylan ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Inhibition Effect ◽  
Carbonic Anhydrase I ◽  
In Vitro Inhibition ◽  
Erythrocyte Carbonic Anhydrase

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

2014 ◽  
Vol 33 (2) ◽  
pp. 199 ◽  
Author(s):  
Hülya Demirhan ◽  
Mustafa Arslan ◽  
Mustafa Oguzhan Kaya ◽  
Yeşim Kaya ◽  
Nahit Gençer ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Human Erythrocytes ◽  
Affinity Column ◽  
Inhibitory Effects ◽  
Thiourea Derivatives ◽  
Carbonic Anhydrase I ◽  
In Vitro Inhibition ◽  
Human Carbonic Anhydrase ◽  
Sepharose 4B

<p>In this study, 9-benzylidene-9<em>H</em>-fluorene-substituted urea (<strong>5a–p</strong>) and thiourea derivatives <strong>(5q–v)</strong> 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, <strong>5f</strong><strong> </strong>was found to be the most active (IC<sub>50</sub> = 21.4 μM) for inhibition of hCA I and <strong>5s </strong>was the most active (IC<sub>50</sub> = 25.3 μM) for inhibition of<strong> </strong>hCA II.</p><p><strong><br /></strong></p>

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