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BioMed Research International
Volume 2014, Article ID 594879, 8 pages
http://dx.doi.org/10.1155/2014/594879
Research Article

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

1Department of Chemistry, Faculty of Art and Sciences, Sakarya University, 54140 Sakarya, Turkey
2Pamukova Vocational High School, Sakarya University, 54900 Sakarya, Turkey
3Department of Chemistry, Faculty of Art and Sciences, Balikesir University, 10145 Balikesir, Turkey

Received 21 February 2014; Revised 13 June 2014; Accepted 8 July 2014; Published 4 August 2014

Academic Editor: Anna Di Fiore

Copyright © 2014 Hilal Kuday et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Abstract

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 ( µM) was found to be the most active compound for hCA I inhibitory activity and 5g ( 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.