| Literature DB >> 27862205 |
Kadir Aksu1, Bünyamin Özgeriş2,3, Parham Taslimi3, Ali Naderi3, İlhami Gülçin3,4, Süleyman Göksu3.
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 Ki 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 Ki 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.Entities:
Keywords: Acetylcholinesterase; Butyrylcholinesterase; Carbonic anhydrase; Enzyme inhibition; Urea
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Year: 2016 PMID: 27862205 DOI: 10.1002/ardp.201600183
Source DB: PubMed Journal: Arch Pharm (Weinheim) ISSN: 0365-6233 Impact factor: 3.751