101. Discovery of Potent Carbonic Anhydrase and Acetylcholinesterase Inhibitors: 2-Aminoindan β-Lactam Derivatives
- Author
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İlhami Gülçin, Zeynep Köksal, Mustafa Zengin, Umit M. Kocyigit, Nastaran Sadeghian, Hasan Özdemir, Hayriye Genç, Ramazan Kalin, [Genc, Hayriye -- Zengin, Mustafa] Sakarya Univ, Fac Arts & Sci, Dept Chem, TR-54050 Sakarya, Turkey -- [Kalin, Ramazan] Erzurum Tech Univ, Dept Basic Sci, Fac Sci, TR-25700 Erzurum, Turkey -- [Koksal, Zeynep] Istanbul Medeniyet Univ, Dept Chem, Fac Sci, TR-34730 Istanbul, Turkey -- [Sadeghian, Nastaran -- Gulcin, Ilhami] Ataturk Univ, Dept Chem, Fac Sci, TR-25240 Erzurum, Turkey -- [Kocyigit, Umit M.] Cumhuriyet Univ, Vocat Sch Hlth Serv, TR-58140 Sivas, Turkey -- [Gulcin, Ilhami] King Saud Univ, Dept Zool, Coll Sci, Riyadh 11451, Saudi Arabia, GULCIN, Ilhami -- 0000-0001-5993-1668, Genc, H, Kalin, R, Koksal, Z, Sadeghian, N, Kocyigit, UM, Zengin, M, Gulcin, I, Ozdemir, H, Sakarya Üniversitesi/Fen-Edebiyat Fakültesi/Kimya Bölümü, Genç Bilgiçli, Hayriye, and Zengin, Mustafa
- Subjects
β-lactam ,Antibiotics ,carbonic anhydrase ,enzyme purification ,01 natural sciences ,Chloride ,lcsh:Chemistry ,chemistry.chemical_compound ,polycyclic compounds ,Carbonic Anhydrase Inhibitors ,enzyme inhibition ,lcsh:QH301-705.5 ,Spectroscopy ,Carbonic Anhydrases ,Neurotransmitter Agents ,biology ,acetylcholinesterase ,General Medicine ,Acetylcholinesterase ,Computer Science Applications ,Chemistry ,Biochemistry ,Indans ,2-azetidinone ,Lactam ,language ,beta-lactam ,medicine.drug ,medicine.drug_class ,Aché ,Stereochemistry ,beta-Lactams ,Isozyme ,Article ,Catalysis ,Inorganic Chemistry ,Carbonic anhydrase ,medicine ,biochemistry ,Humans ,Physical and Theoretical Chemistry ,Carbonic Anhydrase I ,Molecular Biology ,Inhibitory effect ,010405 organic chemistry ,Organic Chemistry ,Acetylcholine ,language.human_language ,0104 chemical sciences ,010404 medicinal & biomolecular chemistry ,lcsh:Biology (General) ,lcsh:QD1-999 ,chemistry ,biology.protein ,Azetidines ,Cholinesterase Inhibitors - Abstract
WOS: 000387768300031, beta-Lactams are pharmacologically important compounds because of their various biological uses, including antibiotic and so on. beta-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 beta-lactams are inhibitors of hCA I, II and AChE. The Ki values of beta-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 beta-lactams (2a-k) inhibit both carbonic anhydrases (CA) isoenzymes and AChE at low nanomolar concentrations., Sakarya University [BAPK-2012-02-04-031], We gratefully acknowledge the partial financial support for this research project from Sakarya University BAPK-2012-02-04-031.
- Published
- 2016
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