Microwave assisted solvent-free mannich bases: synthesis, characterization and effects of these compounds on HCA I and HCA II isozymes

Mannich bases (2a–d) of aromatic amines were synthesized by using a conventional microwave technique under solvent-free conditions and characterized by IR and NMR (1H and 13C) and elemental analysis. The inhibitory effects of the synthesized Mannich bases were examined in vitro by using hydratase a...

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Main Authors: Bülent Büyükkıdan, Nurgün Büyükkıdan, Metin Bülbül, Melek Yılmaz, Evren Derrun Arslanbay, Ekrem Tunca
Format: Article
Language:English
Published: Society of Chemists and Technologists of Macedonia 2021-05-01
Series:Macedonian Journal of Chemistry and Chemical Engineering
Subjects:
Online Access:https://mjcce.org.mk/index.php/MJCCE/article/view/1968
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author Bülent Büyükkıdan
Nurgün Büyükkıdan
Metin Bülbül
Melek Yılmaz
Evren Derrun Arslanbay
Ekrem Tunca
author_facet Bülent Büyükkıdan
Nurgün Büyükkıdan
Metin Bülbül
Melek Yılmaz
Evren Derrun Arslanbay
Ekrem Tunca
author_sort Bülent Büyükkıdan
collection DOAJ
description Mannich bases (2a–d) of aromatic amines were synthesized by using a conventional microwave technique under solvent-free conditions and characterized by IR and NMR (1H and 13C) and elemental analysis. The inhibitory effects of the synthesized Mannich bases were examined in vitro by using hydratase and esterase assays on carbonic anhydrase I and II isozymes (hCA, EC 4.2.1.1) purified from human erythrocyte cells. Acetazolamide was used as the control compound. The values of IC50, the half-maximum inhibitory concentration, were found for hydratase and esterase activities. Only two compounds (2b and 2d) exhibited poor hCA I and hCA II inhibition effects on esterase activity. In contrast, compounds 2a and 2c could be used as carbonic anhydrase activators as a result of the increased esterase activity of hCA I and hCA II isozymes.
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spelling doaj.art-a817beebac3644138f611fdf2c1b700e2022-12-21T21:10:10ZengSociety of Chemists and Technologists of MacedoniaMacedonian Journal of Chemistry and Chemical Engineering1857-55521857-56252021-05-0140110.20450/mjcce.2021.19681573Microwave assisted solvent-free mannich bases: synthesis, characterization and effects of these compounds on HCA I and HCA II isozymesBülent Büyükkıdan0Nurgün Büyükkıdan1Metin Bülbül2Melek Yılmaz3Evren Derrun Arslanbay4Ekrem Tunca5Department of Chemistry, Faculty of Arts and Sciences, Kutahya Dumlupınar University, 43100 Kütahya, TurkeyDepartment of Chemistry, Faculty of Arts and Sciences, Kutahya Dumlupınar University, 43100 KütahyaDepartment of Biohemistry, Faculty of Arts and Sciences, Kutahya Dumlupınar University, 43100 KütahyaDepartment of Chemistry, Faculty of Arts and Sciences, Kutahya Dumlupınar University, 43100 KütahyaDepartment of Chemistry, Faculty of Arts and Sciences, Kutahya Dumlupınar University, 43100 KütahyaDepartment of Biohemistry, Faculty of Arts and Sciences, Kutahya Dumlupınar University, 43100 Kütahya Mannich bases (2a–d) of aromatic amines were synthesized by using a conventional microwave technique under solvent-free conditions and characterized by IR and NMR (1H and 13C) and elemental analysis. The inhibitory effects of the synthesized Mannich bases were examined in vitro by using hydratase and esterase assays on carbonic anhydrase I and II isozymes (hCA, EC 4.2.1.1) purified from human erythrocyte cells. Acetazolamide was used as the control compound. The values of IC50, the half-maximum inhibitory concentration, were found for hydratase and esterase activities. Only two compounds (2b and 2d) exhibited poor hCA I and hCA II inhibition effects on esterase activity. In contrast, compounds 2a and 2c could be used as carbonic anhydrase activators as a result of the increased esterase activity of hCA I and hCA II isozymes. https://mjcce.org.mk/index.php/MJCCE/article/view/1968Activatorcarbonic anhydraseglaucomaisozyme
spellingShingle Bülent Büyükkıdan
Nurgün Büyükkıdan
Metin Bülbül
Melek Yılmaz
Evren Derrun Arslanbay
Ekrem Tunca
Microwave assisted solvent-free mannich bases: synthesis, characterization and effects of these compounds on HCA I and HCA II isozymes
Macedonian Journal of Chemistry and Chemical Engineering
Activator
carbonic anhydrase
glaucoma
isozyme
title Microwave assisted solvent-free mannich bases: synthesis, characterization and effects of these compounds on HCA I and HCA II isozymes
title_full Microwave assisted solvent-free mannich bases: synthesis, characterization and effects of these compounds on HCA I and HCA II isozymes
title_fullStr Microwave assisted solvent-free mannich bases: synthesis, characterization and effects of these compounds on HCA I and HCA II isozymes
title_full_unstemmed Microwave assisted solvent-free mannich bases: synthesis, characterization and effects of these compounds on HCA I and HCA II isozymes
title_short Microwave assisted solvent-free mannich bases: synthesis, characterization and effects of these compounds on HCA I and HCA II isozymes
title_sort microwave assisted solvent free mannich bases synthesis characterization and effects of these compounds on hca i and hca ii isozymes
topic Activator
carbonic anhydrase
glaucoma
isozyme
url https://mjcce.org.mk/index.php/MJCCE/article/view/1968
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