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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...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2016
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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. |
format | Online Article Text |
id | pubmed-5085765 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2016 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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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