Antioxidant Activity, Acetylcholinesterase, and Carbonic Anhydrase Inhibitory Properties of Novel Ureas Derived from Phenethylamines
ARCHIV DER PHARMAZIE, cilt.349, sa.12, ss.944-954, 2016 (SCI-Expanded, Scopus)
- 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.