Antioxidant Activity, Acetylcholinesterase, and Carbonic Anhydrase Inhibitory Properties of Novel Ureas Derived from Phenethylamines. Issue 12 (10th November 2016)

• Record Type: Journal Article
• Authors: Aksu, Kadir; Özgeriş, Bünyamin; Taslimi, Parham; Naderi, Ali; Gülçin, İlhami; Göksu, Süleyman
• Is Part Of: Archiv der Pharmazie. Volume 349:Issue 12(2016)
• Page Start: 944
• Page End: 954
• Publication Date: 2016-11-10
• Subjects: Acetylcholinesterase -- Butyrylcholinesterase -- Carbonic anhydrase -- Enzyme inhibition -- Urea; Pharmaceutical chemistry -- Periodicals; Pharmacology -- Periodicals; 615.19
• DOI: 10.1002/ardp.201600183
• Languages: English
• ISSNs: 0365-6233

Abstract

Abstract : 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 0.307–0.432 nM for hCA I and 0.149–0.278 nM 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. Abstract : A series of urea derivatives were synthesized and assayed for their antioxidant activities and acetylcholinesterase, butyrylcholinesterase, and carbonic anhydrase inhibitory properties. All synthesized compounds showed significant inhibition profiles against these enzymes. Phenolic urea derivatives were demonstrated to be antioxidant agents.