Synthesis and carbonic anhydrase inhibitory properties of novel coumarin derivatives
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, cilt.28, sa.2, ss.299-304, 2013 (SCI-Expanded)
- Yayın Türü: Makale / Tam Makale
- Cilt numarası: 28 Sayı: 2
- Basım Tarihi: 2013
- Doi Numarası: 10.3109/14756366.2012.677838
- Dergi Adı: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
- Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED)
- Sayfa Sayıları: ss.299-304
- Anahtar Kelimeler: Carbonic anhydrase, coumarin, benzimidazolium, inhibition, IN-VITRO INHIBITION, HETEROCYCLIC SULFONAMIDES, AROMATIC/HETEROCYCLIC SULFONAMIDES, SULFAMATE INHIBITORS, HUMAN SERUM, PURIFICATION, TARGET, PARAOXONASE, PESTICIDES, ACTIVATORS
- İnönü Üniversitesi Adresli: Evet
Özet
A newly series of water-soluble 1-alkyl-3-(4-methyl-7, 8-dihydroxy-2H-chromen-2-one) benzimidazolium chloride salts (3a-j) were synthesized and their inhibitory effects on the activity of purified human carbonic anhydrase (hCA) I and II were evaluated. hCA I and II from human erythrocytes were purified by a simple one step procedure by using Sepharose 4B-L-tyrosine-sulphanilamide affinity column. The result showed that all the synthesized compounds were inhibited the CA isoenzymes activity. Among them, 3g and 3j were found to be most active (IC50 = 22.09 mu M and 20.33 mu M) for hCA I and hCA II, respectively.