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

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 CO2 as a substrate. The results showed that all compounds inhibited the hCA I and hCA II enzyme activities. Among all th...

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Bibliographic Details
Published in:BioMed research international 2014-01, Vol.2014 (2014), p.1-8
Main Authors: Kuday, Hilal, Sonmez, Fatih, Bilen, Cigdem, Yavuz, Emre, Gençer, Nahit, Kucukislamoglu, Mustafa
Format: Article
Language:English
Subjects:
Biomedical research
Carbon dioxide
Carbon Dioxide - chemistry
Carbonic Anhydrase I - antagonists & inhibitors
Carbonic Anhydrase I - chemistry
Carbonic Anhydrase I - metabolism
Carbonic Anhydrase II - antagonists & inhibitors
Carbonic Anhydrase II - chemistry
Carbonic Anhydrase II - metabolism
Chalcone - administration & dosage
Chalcone - chemical synthesis
Chemistry
Enzymes
Erythrocytes - enzymology
Healthy Volunteers
Humans
Nonsteroidal anti-inflammatory drugs
Pyrimidines
Pyrimidines - administration & dosage
Pyrimidines - chemical synthesis
Structure-Activity Relationship
Studies
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Summary: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 CO2 as 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 and 5g (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.
ISSN:2314-6133
2314-6141
DOI:10.1155/2014/594879