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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Main Authors:	Hilal Kuday, Fatih Sonmez, Cigdem Bilen, Emre Yavuz, Nahit Gençer, Mustafa Kucukislamoglu
Format:	Article
Language:	English
Published:	Hindawi Limited 2014-01-01
Series:	BioMed Research International
Online Access:	http://dx.doi.org/10.1155/2014/594879

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spelling	doaj-c378013b042a467d9f2df643a50059332020-11-24T23:03:40ZengHindawi LimitedBioMed Research International2314-61332314-61412014-01-01201410.1155/2014/594879594879Synthesis and In Vitro Inhibition Effect of New Pyrido[2,3-d]pyrimidine Derivatives on Erythrocyte Carbonic Anhydrase I and IIHilal Kuday0Fatih Sonmez1Cigdem Bilen2Emre Yavuz3Nahit Gençer4Mustafa Kucukislamoglu5Department of Chemistry, Faculty of Art and Sciences, Sakarya University, 54140 Sakarya, TurkeyPamukova Vocational High School, Sakarya University, 54900 Sakarya, TurkeyDepartment of Chemistry, Faculty of Art and Sciences, Balikesir University, 10145 Balikesir, TurkeyDepartment of Chemistry, Faculty of Art and Sciences, Balikesir University, 10145 Balikesir, TurkeyDepartment of Chemistry, Faculty of Art and Sciences, Balikesir University, 10145 Balikesir, TurkeyDepartment of Chemistry, Faculty of Art and Sciences, Sakarya University, 54140 Sakarya, TurkeyIn 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.http://dx.doi.org/10.1155/2014/594879
collection	DOAJ
language	English
format	Article
sources	DOAJ
author	Hilal Kuday Fatih Sonmez Cigdem Bilen Emre Yavuz Nahit Gençer Mustafa Kucukislamoglu
spellingShingle	Hilal Kuday Fatih Sonmez Cigdem Bilen Emre Yavuz Nahit Gençer Mustafa Kucukislamoglu Synthesis and In Vitro Inhibition Effect of New Pyrido[2,3-d]pyrimidine Derivatives on Erythrocyte Carbonic Anhydrase I and II BioMed Research International
author_facet	Hilal Kuday Fatih Sonmez Cigdem Bilen Emre Yavuz Nahit Gençer Mustafa Kucukislamoglu
author_sort	Hilal Kuday
title	Synthesis and In Vitro Inhibition Effect of New Pyrido[2,3-d]pyrimidine Derivatives on Erythrocyte Carbonic Anhydrase I and II
title_short	Synthesis and In Vitro Inhibition Effect of New Pyrido[2,3-d]pyrimidine Derivatives on Erythrocyte Carbonic Anhydrase I and II
title_full	Synthesis and In Vitro Inhibition Effect of New Pyrido[2,3-d]pyrimidine Derivatives on Erythrocyte Carbonic Anhydrase I and II
title_fullStr	Synthesis and In Vitro Inhibition Effect of New Pyrido[2,3-d]pyrimidine Derivatives on Erythrocyte Carbonic Anhydrase I and II
title_full_unstemmed	Synthesis and In Vitro Inhibition Effect of New Pyrido[2,3-d]pyrimidine Derivatives on Erythrocyte Carbonic Anhydrase I and II
title_sort	synthesis and in vitro inhibition effect of new pyrido[2,3-d]pyrimidine derivatives on erythrocyte carbonic anhydrase i and ii
publisher	Hindawi Limited
series	BioMed Research International
issn	2314-6133 2314-6141
publishDate	2014-01-01
description	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.
url	http://dx.doi.org/10.1155/2014/594879
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Synthesis and In Vitro Inhibition Effect of New Pyrido[2,3-d]pyrimidine Derivatives on Erythrocyte Carbonic Anhydrase I and II

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