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Synthesis and carbonic anhydrase inhibitory properties of novel 1,4-dihydropyrimidinone substituted diarylureas

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dc.creator Demir, Dudu
dc.creator Celik, Fatma
dc.creator Gencer, Nahit
dc.creator Yavuz, Emre
dc.creator Arslan, Mustafa
dc.date 2014-01-31T22:00:00Z
dc.date.accessioned 2020-10-06T12:03:28Z
dc.date.available 2020-10-06T12:03:28Z
dc.identifier fcf903a1-1406-4d70-a254-da62665462fa
dc.identifier 10.3109/14756366.2012.746972
dc.identifier https://avesis.sdu.edu.tr/publication/details/fcf903a1-1406-4d70-a254-da62665462fa/oai
dc.identifier.uri http://acikerisim.sdu.edu.tr/xmlui/handle/123456789/77041
dc.description A new series of 1,4-dihydropyrimidinone (DHPM) substituted diaryl urea and thiourea derivatives were synthesized and their inhibitory effects on the activity of purified human carbonic anhydrase (hCA) I and II were evaluated. 4-Nitrophenyl-1,4-DHPM was prepared with dimedone, nitrobenzaldehyde and urea or thiourea and nitro group was reduced to amine derivative. The compound was reacted with isocyanates and isothiocyanates to get the final products. The results showed that all the synthesized compounds inhibited the carbonic anhydrase isoenzyme activity; 4c (IC50 = 66.23 mu M for hCA I) and 4f (IC50 = 63.09 mu M for hCA II) have the most inhibitory effect. The synthesized compounds are very bulky to be able to bind near the zinc ion and they much more probably bind as the coumarins and activators.
dc.language eng
dc.rights info:eu-repo/semantics/closedAccess
dc.title Synthesis and carbonic anhydrase inhibitory properties of novel 1,4-dihydropyrimidinone substituted diarylureas
dc.type info:eu-repo/semantics/article


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