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

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...

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Autores principales: Genç, Hayriye, Kalin, Ramazan, Köksal, Zeynep, Sadeghian, Nastaran, Kocyigit, Umit M., Zengin, Mustafa, Gülçin, İlhami, Özdemir, Hasan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5085765/
https://www.ncbi.nlm.nih.gov/pubmed/27775608
http://dx.doi.org/10.3390/ijms17101736
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author Genç, Hayriye
Kalin, Ramazan
Köksal, Zeynep
Sadeghian, Nastaran
Kocyigit, Umit M.
Zengin, Mustafa
Gülçin, İlhami
Özdemir, Hasan
author_facet Genç, Hayriye
Kalin, Ramazan
Köksal, Zeynep
Sadeghian, Nastaran
Kocyigit, Umit M.
Zengin, Mustafa
Gülçin, İlhami
Özdemir, Hasan
author_sort Genç, Hayriye
collection PubMed
description 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 K(i) values 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.
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spelling pubmed-50857652016-11-01 Discovery of Potent Carbonic Anhydrase and Acetylcholinesterase Inhibitors: 2-Aminoindan β-Lactam Derivatives Genç, Hayriye Kalin, Ramazan Köksal, Zeynep Sadeghian, Nastaran Kocyigit, Umit M. Zengin, Mustafa Gülçin, İlhami Özdemir, Hasan Int J Mol Sci Article 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 K(i) values 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. MDPI 2016-10-20 /pmc/articles/PMC5085765/ /pubmed/27775608 http://dx.doi.org/10.3390/ijms17101736 Text en © 2016 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC-BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Genç, Hayriye
Kalin, Ramazan
Köksal, Zeynep
Sadeghian, Nastaran
Kocyigit, Umit M.
Zengin, Mustafa
Gülçin, İlhami
Özdemir, Hasan
Discovery of Potent Carbonic Anhydrase and Acetylcholinesterase Inhibitors: 2-Aminoindan β-Lactam Derivatives
title Discovery of Potent Carbonic Anhydrase and Acetylcholinesterase Inhibitors: 2-Aminoindan β-Lactam Derivatives
title_full Discovery of Potent Carbonic Anhydrase and Acetylcholinesterase Inhibitors: 2-Aminoindan β-Lactam Derivatives
title_fullStr Discovery of Potent Carbonic Anhydrase and Acetylcholinesterase Inhibitors: 2-Aminoindan β-Lactam Derivatives
title_full_unstemmed Discovery of Potent Carbonic Anhydrase and Acetylcholinesterase Inhibitors: 2-Aminoindan β-Lactam Derivatives
title_short Discovery of Potent Carbonic Anhydrase and Acetylcholinesterase Inhibitors: 2-Aminoindan β-Lactam Derivatives
title_sort discovery of potent carbonic anhydrase and acetylcholinesterase inhibitors: 2-aminoindan β-lactam derivatives
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5085765/
https://www.ncbi.nlm.nih.gov/pubmed/27775608
http://dx.doi.org/10.3390/ijms17101736
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