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Antioxidant Activity, Acetylcholinesterase, and Carbonic Anhydrase Inhibitory Properties of Novel Ureas Derived from Phenethylamines.
Arch Pharm (Weinheim). 2016 Dec; 349(12):944-954.AP

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.

Authors+Show Affiliations

Faculty of Arts and Sciences, Department of Chemistry, Ordu University, Ordu, Turkey.Faculty of Science, Department of Basic Sciences, Erzurum Technical University, Erzurum, Turkey. Faculty of Science, Department of Chemistry, Ataturk University, Erzurum, Turkey.Faculty of Science, Department of Chemistry, Ataturk University, Erzurum, Turkey.Faculty of Science, Department of Chemistry, Ataturk University, Erzurum, Turkey.Faculty of Science, Department of Chemistry, Ataturk University, Erzurum, Turkey. Department of Zoology, College of Science, King Saud University, Riyadh, Saudi Arabia.Faculty of Science, Department of Chemistry, Ataturk University, Erzurum, Turkey.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

27862205

Citation

Aksu, Kadir, et al. "Antioxidant Activity, Acetylcholinesterase, and Carbonic Anhydrase Inhibitory Properties of Novel Ureas Derived From Phenethylamines." Archiv Der Pharmazie, vol. 349, no. 12, 2016, pp. 944-954.
Aksu K, Özgeriş B, Taslimi P, et al. Antioxidant Activity, Acetylcholinesterase, and Carbonic Anhydrase Inhibitory Properties of Novel Ureas Derived from Phenethylamines. Arch Pharm (Weinheim). 2016;349(12):944-954.
Aksu, K., Özgeriş, B., Taslimi, P., Naderi, A., Gülçin, İ., & Göksu, S. (2016). Antioxidant Activity, Acetylcholinesterase, and Carbonic Anhydrase Inhibitory Properties of Novel Ureas Derived from Phenethylamines. Archiv Der Pharmazie, 349(12), 944-954. https://doi.org/10.1002/ardp.201600183
Aksu K, et al. Antioxidant Activity, Acetylcholinesterase, and Carbonic Anhydrase Inhibitory Properties of Novel Ureas Derived From Phenethylamines. Arch Pharm (Weinheim). 2016;349(12):944-954. PubMed PMID: 27862205.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Antioxidant Activity, Acetylcholinesterase, and Carbonic Anhydrase Inhibitory Properties of Novel Ureas Derived from Phenethylamines. AU - Aksu,Kadir, AU - Özgeriş,Bünyamin, AU - Taslimi,Parham, AU - Naderi,Ali, AU - Gülçin,İlhami, AU - Göksu,Süleyman, Y1 - 2016/11/10/ PY - 2016/06/22/received PY - 2016/10/18/revised PY - 2016/10/21/accepted PY - 2016/11/20/pubmed PY - 2017/4/22/medline PY - 2016/11/19/entrez KW - Acetylcholinesterase KW - Butyrylcholinesterase KW - Carbonic anhydrase KW - Enzyme inhibition KW - Urea SP - 944 EP - 954 JF - Archiv der Pharmazie JO - Arch. Pharm. (Weinheim) VL - 349 IS - 12 N2 - 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. SN - 1521-4184 UR - https://www.unboundmedicine.com/medline/citation/27862205/Antioxidant_Activity_Acetylcholinesterase_and_Carbonic_Anhydrase_Inhibitory_Properties_of_Novel_Ureas_Derived_from_Phenethylamines_ L2 - https://doi.org/10.1002/ardp.201600183 DB - PRIME DP - Unbound Medicine ER -