Synthesis and in vitro inhibition effect of new pyrido[2,3-d]pyrimidine derivatives on erythrocyte carbonic anhydrase i and II

Kuday H., Sonmez F., BİLEN Ç., Yavuz E., Gençer N., Kucukislamoglu M.

BioMed Research International, cilt.2014, 2014 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 2014
  • Basım Tarihi: 2014
  • Doi Numarası: 10.1155/2014/594879
  • Dergi Adı: BioMed Research International
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • İstanbul Yeni Yüzyıl Üniversitesi Adresli: Hayır

Özet

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 COas 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.