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 CO(2) as a substrate. The results showed that all compounds inhibited the hCA I and hCA II enzyme activities. Among all...

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Detalles Bibliográficos
Autores principales: Kuday, Hilal, Sonmez, Fatih, Bilen, Cigdem, Yavuz, Emre, Gençer, Nahit, Kucukislamoglu, Mustafa
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Hindawi Publishing Corporation 2014
Materias:
Research Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4139024/
https://www.ncbi.nlm.nih.gov/pubmed/25165709
http://dx.doi.org/10.1155/2014/594879
Descripción
Sumario: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 CO(2) as a substrate. The results showed that all compounds inhibited the hCA I and hCA II enzyme activities. Among all the synthesized compounds, 7e (IC(50) = 6.79 µM) was found to be the most active compound for hCA I inhibitory activity and 5g (IC(50) = 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.

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