title: Discovery of Potent Carbonic Anhydrase and Acetylcholinesterase Inhibitors: 2-Aminoindan β-Lactam Derivatives.
abstract: β-Lactams are pharmacologically important compounds because of their various biological uses, including antibiotic and so on. β-Lactams were synthesized from benzylidene-inden derivatives and acetoxyacetyl chloride. The inhibitory effect of these compounds was examined for human carbonic anhydrase I and II (hCA I, and II) and acetylcholinesterase (AChE). The results reveal that β-lactams are inhibitors of hCA I, II and AChE. TheKivalues of β-lactams (2a-k) were 0.44-6.29 nM against hCA I, 0.93-8.34 nM against hCA II, and 0.25-1.13 nM against AChE. Our findings indicate that β-lactams (2a-k) inhibit both carbonic anhydrases (CA) isoenzymes and AChE at low nanomolar concentrations.
authors: Department of Chemistry, Faculty of Arts and Sciences, Sakarya University, Sakarya 54050, Turkey. hayriyegenc@sakarya.edu.tr.
authors: Hayriye
authors: H
authors: Genç
authors: Department of Basic Science, Faculty of Science, Erzurum Technical University, Erzurum 25700, Turkey. rkalin@atauni.edu.tr.
authors: Ramazan
authors: R
authors: Kalin
authors: Department of Chemistry, Faculty of Sciences, İstanbul Medeniyet University, İstanbul 34730, Turkey. zkoksal@atauni.edu.tr.
authors: Zeynep
authors: Z
authors: Köksal
authors: Department of Chemistry, Faculty of Science, Atatürk University, Erzurum 25240, Turkey. parham_taslimi_un@yahoo.com.
authors: Nastaran
authors: N
authors: Sadeghian
authors: Vocational School of Health Services, Cumhuriyet University, Sivas 58140, Turkey. ukocyigit@cumhuriyet.edu.tr.
authors: Umit M
authors: UM
authors: Kocyigit
authors: Department of Chemistry, Faculty of Arts and Sciences, Sakarya University, Sakarya 54050, Turkey. mzengin@sakarya.edu.tr.
authors: Mustafa
authors: M
authors: Zengin
authors: Department of Chemistry, Faculty of Science, Atatürk University, Erzurum 25240, Turkey. igulcin@atauni.edu.tr.|Department of Zoology, College of Science, King Saud University, Riyadh 11451, Saudi Arabia. igulcin@atauni.edu.tr.
authors: İlhami
authors: İ
authors: Gülçin
authors: Department of Chemistry, Faculty of Science, Atatürk University, Erzurum 25240, Turkey. hozdemir@atauni.edu.tr.
authors: Hasan
authors: H
authors: Özdemir
mesh_terms: D000109:Acetylcholine / Q000378:metabolism; D000110:Acetylcholinesterase / Q000378:metabolism*; D001384:Azetidines / Q000737:chemistry; D002257:Carbonic Anhydrase Inhibitors / Q000737:chemistry*; D002256:Carbonic Anhydrases / Q000378:metabolism*; D002800:Cholinesterase Inhibitors / Q000737:chemistry*; D006801:Humans; D007189:Indans / Q000737:chemistry; D018377:Neurotransmitter Agents / Q000378:metabolism; D047090:beta-Lactams / Q000737:chemistry*
chemical_list: C116379:2-azetidinone; D001384:Azetidines; D002257:Carbonic Anhydrase Inhibitors; D002800:Cholinesterase Inhibitors; D007189:Indans; D018377:Neurotransmitter Agents; D047090:beta-Lactams; C006545:2-aminoindan; D000110:Acetylcholinesterase; D002256:Carbonic Anhydrases; D000109:Acetylcholine
keywords: 2-azetidinone; acetylcholinesterase; carbonic anhydrase; enzyme inhibition; enzyme purification; β-lactam