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

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dc.contributor.author Kucukoglu, Kaan
dc.contributor.author Gul, Halise Inci
dc.contributor.author Taslimi, Parham
dc.contributor.author Gulcin, Ilhami
dc.contributor.author Supuran, Claudiu T.
dc.date.accessioned 2019-04-29T07:33:46Z
dc.date.available 2019-04-29T07:33:46Z
dc.date.issued 2019-02-04
dc.identifier.uri http://hdl.handle.net/11772/1118
dc.description.abstract Recently, 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 Ki 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)propylidene]hydrazine dihydrochlorides, P4, in P-series, and N,N′-bis[1-(4-chlorophenyl)-3-(pyrrolidine-1-yl)propylidene]hydrazine dihydrochlorides, R5, in R-series were the most powerful compounds against hCA I with the Ki 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 Ki 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 Ki 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 Ki 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 Ki values of 119 ± 20 nM, 88 ± 14 nM, respectively. en_US
dc.language.iso eng en_US
dc.publisher Bioorganic Chemistry en_US
dc.relation.isversionof https://doi.org/10.1016/j.bioorg.2019.02.008 en_US
dc.rights info:eu-repo/semantics/restrictedAccess en_US
dc.subject Hydrazone en_US
dc.subject Mannich base en_US
dc.subject Carbonic anhydrase en_US
dc.subject Acetylcholinesterase en_US
dc.subject Enzyme inhibition en_US
dc.title Investigation of inhibitory properties of some hydrazone compounds on hCA I, hCA II and AChE enzymes en_US
dc.type article en_US
dc.relation.journal Bioorganic Chemistry en_US
dc.identifier.volume 86 en_US
dc.identifier.startpage 316 en_US
dc.identifier.endpage 321 en_US


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