Inhibitory effects of isatin Mannich bases on carbonic anhydrases, acetylcholinesterase, and butyrylcholinesterase

Autor:	Dilan Ozmen Ozgun, Telat Yanik, İlhami Gülçin, Claudiu T. Supuran, Cem Yamali, Halise Inci Gul, Parham Taslimi
Přispěvatelé:	Belirlenecek, GULCIN, Ilhami -- 0000-0001-5993-1668, YANIK, Telat -- 0000-0003-0975-0281, Gul, Halise Inci -- 0000-0001-6164-9602, Yamali, Cem -- 0000-0002-4833-7900, Bartın Üniversitesi, Fen Fakültesi, Biyoteknoloji Bölümü
Rok vydání:	2016
Předmět:	Stereochemistry Proton Magnetic Resonance Spectroscopy carbonic anhydrase isatin 01 natural sciences Isozyme chemistry.chemical_compound Carbonic anhydrase Drug Discovery medicine Carbonic Anhydrase Inhibitors Butyrylcholinesterase Carbonic Anhydrases Cholinesterase Pharmacology chemistry.chemical_classification biology 010405 organic chemistry Isatin General Medicine Acetylcholinesterase 0104 chemical sciences 010404 medicinal & biomolecular chemistry Enzyme chemistry Biochemistry Mannich bases Tacrine butyrylcholinesterase biology.protein Cholinesterase Inhibitors medicine.drug
Zdroj:	Journal of Enzyme Inhibition and Medicinal Chemistry. 31:1498-1501
ISSN:	1475-6374 1475-6366
Popis:	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. Research Foundation of Agri Ibrahim Cecen University, Turkey [FEF.14.009] This study was supported by the Research Foundation of Agri Ibrahim Cecen University, Turkey, Project No: FEF.14.009.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5ea267cbc9799b5ce7b9ed55d0ebe079 https://doi.org/10.3109/14756366.2016.1149479 Zobrazit plný text záznamu Plný text ve formátu PDF Plný text ve formátu HTML
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