Antioxidant Activity, Acetylcholinesterase, and Carbonic Anhydrase Inhibitory Properties of Novel Ureas Derived from Phenethylamines

Aksu K., Ozgeris B., TASLIMI P., NADERI A., GÜLÇİN İ., GÖKSU S.

ARCHIV DER PHARMAZIE, cilt.349, sa.12, ss.944-954, 2016 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 349 Sayı: 12
  • Basım Tarihi: 2016
  • Doi Numarası: 10.1002/ardp.201600183
  • Dergi Adı: ARCHIV DER PHARMAZIE
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.944-954
  • Anahtar Kelimeler: Acetylcholinesterase, Butyrylcholinesterase, Carbonic anhydrase, Enzyme inhibition, Urea, LYOPHILIZED AQUEOUS EXTRACT, GLUTATHIONE-S-TRANSFERASE, ISOENZYMES HCA I, POLYPHENOL CONTENTS, CAFFEIC ACID, ANTIRADICAL ACTIVITIES, PHENOLIC-COMPOUNDS, POTENT INHIBITOR, ESTER CAPE, DERIVATIVES
  • Atatürk Üniversitesi Adresli: Evet

Özet

A series of ureas derived from phenethylamines were synthesized and evaluated for human carbonic anhydrase (hCA) I and II, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) enzyme inhibitory activities and antioxidant properties. The ureas were synthesized from the reactions of substituted phenethylamines with N,N-dimethylcarbamoyl chloride; then, the synthesized compounds were converted to their corresponding phenolic derivatives via O-demethylation. hCA I and II were effectively inhibited by the newly synthesized compounds, with K-i values in the range of 0.307-0.432nM for hCA I and 0.149-0.278nM for hCA II. On the other hand, the K-i parameters of these compounds for AChE and BChE were determined in the range of 0.129-0.434 and 0.095-0.207 nM, respectively. Phenolic ureas also showed good antioxidant activities.