Inhibitory effects of isatin Mannich bases on carbonic anhydrases,acetylcholinesterase, and butyrylcholinesterase |
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| Authors: | Dilan Ozmen Ozgun Cem Yamali Parham Taslimi Ilhami Gulcin |
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| Institution: | 1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Agri Ibrahim Cecen University, Agri, Turkey,;2. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ataturk University, Erzurum, Turkey,;3. Department of Chemistry, Faculty of Science, Ataturk University, Erzurum, Turkey,;4. Department of Chemistry, Faculty of Science, Ataturk University, Erzurum, Turkey,;5. Department of Zoology, College of Science, King Saud University, Riyadh, Saudi Arabia, |
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| Abstract: | The effects of isatin Mannich bases incorporating (1-piperidin-1-yl (P1)/morpholin-4-yl (P2)/N-methylpiperazin-1-yl (P3)]methyl)-1H-indole-2,3-dione) moieties against human (h) carbonic anhydrase (CA, EC 4.2.1.1) isoenzymes hCA I and hCA II, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) enzymes were evaluated. P1–P3 demonstrated impressive inhibition profiles against AChE and BChE and also inhibited both CAs at nanomolar level. These inhibitory effects were more powerful in all cases than the reference compounds used for all these enzymes. This study suggests that isatin Mannich bases P1–P3 are good candidate compounds especially for the development of new cholinesterase inhibitors since they were 2.2–5.9 times better inhibitors than clinically used drug Tacrine. |
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| Keywords: | Acetylcholinesterase butyrylcholinesterase carbonic anhydrase isatin Mannich bases |
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