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Int. J. Mol. Sci. 2016, 17(10), 1736; doi:10.3390/ijms17101736

Discovery of Potent Carbonic Anhydrase and Acetylcholinesterase Inhibitors: 2-Aminoindan β-Lactam Derivatives

1
Department of Chemistry, Faculty of Arts and Sciences, Sakarya University, Sakarya 54050, Turkey
2
Department of Basic Science, Faculty of Science, Erzurum Technical University, Erzurum 25700, Turkey
3
Department of Chemistry, Faculty of Sciences, İstanbul Medeniyet University, İstanbul 34730, Turkey
4
Department of Chemistry, Faculty of Science, Atatürk University, Erzurum 25240, Turkey
5
Vocational School of Health Services, Cumhuriyet University, Sivas 58140, Turkey
6
Department of Zoology, College of Science, King Saud University, Riyadh 11451, Saudi Arabia
*
Author to whom correspondence should be addressed.
Academic Editor: Mateus Webba da Silva
Received: 17 July 2016 / Revised: 2 October 2016 / Accepted: 10 October 2016 / Published: 20 October 2016
(This article belongs to the Section Biochemistry, Molecular and Cellular Biology)
View Full-Text   |   Download PDF [1230 KB, uploaded 20 October 2016]   |  

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. The Ki values of β-lactams (2ak) 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 (2ak) inhibit both carbonic anhydrases (CA) isoenzymes and AChE at low nanomolar concentrations. View Full-Text
Keywords: carbonic anhydrase; acetylcholinesterase; β-lactam; 2-azetidinone; enzyme inhibition; enzyme purification carbonic anhydrase; acetylcholinesterase; β-lactam; 2-azetidinone; enzyme inhibition; enzyme purification
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MDPI and ACS Style

Genç, H.; Kalin, R.; Köksal, Z.; Sadeghian, N.; Kocyigit, U.M.; Zengin, M.; Gülçin, İ.; Özdemir, H. Discovery of Potent Carbonic Anhydrase and Acetylcholinesterase Inhibitors: 2-Aminoindan β-Lactam Derivatives. Int. J. Mol. Sci. 2016, 17, 1736.

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