title: Inhibitory effects of isatin Mannich bases on carbonic anhydrases, acetylcholinesterase, and butyrylcholinesterase.
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.
authors.affiliation: a Department of Pharmaceutical Chemistry , Faculty of Pharmacy, Agri Ibrahim Cecen University , Agri , Turkey .
authors.forename: Dilan Ozmen
authors.initials: DO
authors.lastname: Ozgun
authors.affiliation: b Department of Pharmaceutical Chemistry , Faculty of Pharmacy, Ataturk University , Erzurum , Turkey .
authors.forename: Cem
authors.initials: C
authors.lastname: Yamali
authors.affiliation: b Department of Pharmaceutical Chemistry , Faculty of Pharmacy, Ataturk University , Erzurum , Turkey .
authors.forename: Halise Inci
authors.initials: HI
authors.lastname: Gul
authors.affiliation: c Department of Chemistry , Faculty of Science, Ataturk University , Erzurum , Turkey .
authors.forename: Parham
authors.initials: P
authors.lastname: Taslimi
authors.affiliation: c Department of Chemistry , Faculty of Science, Ataturk University , Erzurum , Turkey .|d Department of Zoology, College of Science , King Saud University , Riyadh , Saudi Arabia .
authors.forename: Ilhami
authors.initials: I
authors.lastname: Gulcin
authors.affiliation: e Department of Biology, Faculty of Science , Agri Ibrahim Cecen University , Agri , Turkey , and.
authors.forename: Telat
authors.initials: T
authors.lastname: Yanik
authors.affiliation: f Neurofarba Department e Laboratorio di Chimica Bioinorganica, Universita Degli Studi di Firenze , Sesto Fiorentino (Florence) , Italy.
authors.forename: Claudiu T
authors.initials: CT
authors.lastname: Supuran
mesh_terms: D000110:Acetylcholinesterase / Q000378:metabolism*; D002091:Butyrylcholinesterase / Q000378:metabolism*; D002257:Carbonic Anhydrase Inhibitors / Q000494:pharmacology*; D002256:Carbonic Anhydrases / Q000378:metabolism*; D002800:Cholinesterase Inhibitors / Q000494:pharmacology*; D007510:Isatin / Q000494:pharmacology*; D008352:Mannich Bases / Q000737:chemistry*; D066244:Proton Magnetic Resonance Spectroscopy
chemical_list: D002257:Carbonic Anhydrase Inhibitors; D002800:Cholinesterase Inhibitors; D008352:Mannich Bases; D007510:Isatin; D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase; D002256:Carbonic Anhydrases
keywords: Acetylcholinesterase; Mannich bases; butyrylcholinesterase; carbonic anhydrase; isatin