Synthesis, characterization and carbonic anhydrase inhibitory activity of novel benzothiazole derivatives

Küçük Resim Yok

Tarih

2016

Dergi Başlığı

Dergi ISSN

Cilt Başlığı

Yayıncı

Taylor & Francis Ltd

Erişim Hakkı

info:eu-repo/semantics/closedAccess

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.

Açıklama

Anahtar Kelimeler

Amino acid-benzothiazole conjugates, benzothiazole, carbonic anhydrase

Kaynak

Journal of Enzyme Inhibition and Medicinal Chemistry

WoS Q Değeri

Q1

Scopus Q Değeri

Q1

Cilt

31

Sayı

6

Künye