Investigation of inhibitory properties of some hydrazone compounds on hCA I, hCA II and AChE enzymes

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dc.contributor.authorKucukoglu, Kaan
dc.contributor.authorGul, Halise Inci
dc.contributor.authorTaslimi, Parham
dc.contributor.authorGulcin, Ilhami
dc.contributor.authorSupuran, Claudiu T.
dc.date.accessioned2020-03-26T20:14:52Z
dc.date.available2020-03-26T20:14:52Z
dc.date.issued2019
dc.departmentSelçuk Üniversitesi, Eczacılık Fakültesi, Eczacılık Meslek Bilimleri Bölümüen_US
dc.description.abstractRecently, inhibition of carbonic anhydrase (hCA) and acetylcholinesterase (AChE) have appeared as a promising approach for pharmacological intervention in a variety of disorders such as glaucoma, epilepsy, obesity, cancer, and Alzheimer's disease. Keeping this in mind, N, N'-bis[(1-aryl-3-heteroaryl) propylidene] hydrazine dihydrochlorides, N1-N11, P1, P4-P8, and R1-R6, were synthesized to investigate their inhibitory activity against hCA I, hCA II, and AChE enzymes. All compounds in N, P, and R-series inhibited hCAs (I and II) and AChE more efficiently than the reference compounds acetazolamide (AZA), and tacrine. According to the activity results, the most effective inhibitory compounds were in R-series with the K-i values of 203 +/- 55-473 +/- 67 nM and 200 +/- 34-419 +/- 94 nM on hCA I, and hCA II, respectively. N, N'-Bis[1-(4-fluorophenyl)-3-(morpholine-4-yl) propylidene] hydrazine dihydrochlorides, N8, in N-series, N, N'-Bis[1-(4-hydroxyphenyl)-3-(piperidine-1-yl) pro-pylidene] hydrazine dihydrochlorides, P4, in P-series, and N, N'-bis[1-(4-chlorophenyl)-3-(pyrrolidine-1-yl) pro-pylidene] hydrazine dihydrochlorides, R5, in R-series were the most powerful compounds against hCA I with the K-i values of 438 +/- 65 nM, 344 +/- 64 nM, and 203 +/- 55 nM, respectively. Similarly, N8, P4, and R5 efficiently inhibited hCA II isoenzyme with the K-i values of 405 +/- 60 nM, 327 +/- 80 nM, and 200 +/- 34 nM, respectively. On the other hand, P-series compounds had notable inhibitory effect against AChE than the reference compound tacrine and the K-i values were between 66 +/- 20 nM and 128 +/- 36 nM. N, N'-Bis[1-(4-fluorophenyl)-3-(piperidine-1-yl) propylidene] hydrazine dihydrochlorides, P7, was the most potent compound on AChE with the K-i value of 66 +/- 20 nM. The other most promising compounds, N, N'-bis[1-(4-hydroxyphenyl)-3-(morpholine-4-yl) propylidene] hydrazine dihydrochlorides, N4 in N-series and N, N'-bis[1-(4-hydroxyphenyl)-3-(pyrrolidine-1-yl) propylidene] hydrazine dihydrochlorides, R4 in R-series were againts AChE with the K-i values of 119 +/- 20 nM, 88 +/- 14 nM, respectively.en_US
dc.description.sponsorshipResearch Foundation of Ataturk University Erzurum (Turkey)Ataturk Universityen_US
dc.description.sponsorshipThis study was supported by the Research Foundation of Ataturk University Erzurum (Turkey).en_US
dc.identifier.citationKucukoglu, K., Gul, H. I., Taslimi, P., Gulcin, I., Supuran, C. T. (2019). Investigation Of İnhibitory Properties Of Some Hydrazone Compounds On Hca I, Hca II And Ache Enzymes. Bioorganic Chemistry, 86, 316-321.
dc.identifier.doi10.1016/j.bioorg.2019.02.008en_US
dc.identifier.endpage321en_US
dc.identifier.issn0045-2068en_US
dc.identifier.issn1090-2120en_US
dc.identifier.pmid30743172en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.startpage316en_US
dc.identifier.urihttps://dx.doi.org/10.1016/j.bioorg.2019.02.008
dc.identifier.urihttps://hdl.handle.net/20.500.12395/37947
dc.identifier.volume86en_US
dc.identifier.wosWOS:000464108100033en_US
dc.identifier.wosqualityQ1en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.institutionauthorKucukoglu, Kaan
dc.language.isoenen_US
dc.publisherACADEMIC PRESS INC ELSEVIER SCIENCEen_US
dc.relation.ispartofBIOORGANIC CHEMISTRYen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.selcuk20240510_oaigen_US
dc.subjectHydrazoneen_US
dc.subjectMannich baseen_US
dc.subjectCarbonic anhydraseen_US
dc.subjectAcetylcholinesteraseen_US
dc.subjectEnzyme inhibitionen_US
dc.titleInvestigation of inhibitory properties of some hydrazone compounds on hCA I, hCA II and AChE enzymesen_US
dc.typeArticleen_US

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