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Novel benzylic substituted imidazolinium, tetrahydropyrimidinium and tetrahydrodiazepinium salts: potent carbonic anhydrase and acetylcholinesterase inhibitors

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dc.contributor.author Yigit, Beyhan
dc.contributor.author Yigit, Murat
dc.contributor.author Celepci, Duygu Barut
dc.contributor.author Gok, Yetkin
dc.contributor.author Aktas, Aydin
dc.contributor.author Aygun, Muhittin
dc.contributor.author Taslimi, Parham
dc.contributor.author Gulcin, Ilhami Ilhami
dc.date.accessioned 2019-04-29T07:57:00Z
dc.date.available 2019-04-29T07:57:00Z
dc.date.issued 2018-07-23
dc.identifier.uri http://hdl.handle.net/11772/1123
dc.description.abstract The new imidazolinium, tetrahydropyrimidinium and tetrahydrodiazepinium salts were synthesized in good yield by the reaction of the corresponding N,N'-dialkylalkanediamine with triethyl orthoformate in the presence of ammonium chloride. All of the compounds were obtained, and spectroscopically characterized. The crystal structure for the 1,3-bis(4-benzyloxy-3-methoxybenzyl)-3,4,5,6-tetrahydropyrimidinium chloride (5g) was determined by single-crystal X-ray diffraction. The biological properties of all novel compounds were tested and the influence of ring size and benzylic N-substituents on the biological activities were examined. Also, they were found as effective inhibitors against cytosolic carbonic anhydrase I and II isoforms (hCA I and II), and acetylcholinesterase (AChE) enzyme. Among these compounds, 1,3-bis(4-(1-piperidinyl)benzyl)-3,4,5,6-tetrahydropyrimidinium chloride (5f) demonstrated the the best inhibition effects against hCA I, 1,3-bis(4-benzyloxy-3-methoxybenzyl)-3,4,5,6-tetrahydropyrimidinium chloride (5g) demonstrated the the best inhibition effects against cytosolic hCA II isoenzyme. On the other hand, 1,3-Bis(4-methylthiobenzyl)-3,4,5,6-tetrahydropyrimidinium chloride, (5e) demonstrated the the best inhibition effects against AChE enzyme. en_US
dc.language.iso eng en_US
dc.relation.isversionof 10.1002/slct.201801019 en_US
dc.rights info:eu-repo/semantics/restrictedAccess en_US
dc.subject Acetylcholinesterase en_US
dc.subject Carbonic anhydrase en_US
dc.subject Crystal structure en_US
dc.subject Enzyme inhibition en_US
dc.subject Novel imidazolinium en_US
dc.title Novel benzylic substituted imidazolinium, tetrahydropyrimidinium and tetrahydrodiazepinium salts: potent carbonic anhydrase and acetylcholinesterase inhibitors en_US
dc.type article en_US
dc.contributor.department Bartın Üniversitesi, Fen Fakültesi, Biyoteknoloji Bölümü en_US
dc.identifier.volume 3 en_US
dc.identifier.issue 27 en_US
dc.identifier.startpage 7976 en_US
dc.identifier.endpage 7982 en_US


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