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

الملخص EN

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.