Synthesis, characterization and carbonic anhydrase inhibitory activity of novel benzothiazole derivatives
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, cilt.31, sa.6, ss.1221-1225, 2016 (SCI-Expanded, Scopus)
- Yayın Türü: Makale / Tam Makale
- Cilt numarası: 31 Sayı: 6
- Basım Tarihi: 2016
- Doi Numarası: 10.3109/14756366.2015.1114931
- Dergi Adı: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
- Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
- Sayfa Sayıları: ss.1221-1225
- Anahtar Kelimeler: Amino acid-benzothiazole conjugates, benzothiazole, carbonic anhydrase, ANTIMICROBIAL ACTIVITY, DISCOVERY, BIOASSAY, AGENTS, DRUGS
- İnönü Üniversitesi Adresli: Evet
Özet
N-protected amino acids were reacted with substituted benzothiazoles to give the corresponding N-protected amino acid-benzothiazole conjugates (60-89%). Their structures were confirmed by proton nuclear magnetic resonance (H-1 NMR), carbon-13 nuclear magnetic resonance (C-13 NMR), IR and elemental analysis. Their carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activities were determined against two cytosolic human isoforms (hCA I and hCA II), one membrane-associated (hCA IV) and one transmembrane (hCA XII) enzyme by a stopped-flow CO2 hydrase assay method. The new compounds showed rather weak, micromolar inhibitory activity against most of these enzymes.