Synthesis and In Vitro Inhibition Effect of New Pyrido2,3-dpyrimidine Derivatives on Erythrocyte Carbonic Anhydrase I and IIReportar como inadecuado




Synthesis and In Vitro Inhibition Effect of New Pyrido2,3-dpyrimidine Derivatives on Erythrocyte Carbonic Anhydrase I and II - Descarga este documento en PDF. Documentación en PDF para descargar gratis. Disponible también para leer online.

BioMed Research InternationalVolume 2014 2014, Article ID 594879, 8 pages

Research Article

Department of Chemistry, Faculty of Art and Sciences, Sakarya University, 54140 Sakarya, Turkey

Pamukova Vocational High School, Sakarya University, 54900 Sakarya, Turkey

Department 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 pyrido2,3-dpyrimidine 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 pyrido2,3-dpyrimidine derivatives on hCA I and hCA II. Additionally, methyl group bonded to uracil ring increases inhibitory activities on both hCA I and hCA II.





Autor: Hilal Kuday, Fatih Sonmez, Cigdem Bilen, Emre Yavuz, Nahit Gençer, and Mustafa Kucukislamoglu

Fuente: https://www.hindawi.com/



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