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dc.contributor.authorKocyigit, U.M. and Aslan, O.N. and Gulcin, I. and Temel, Y. and Ceylan, M.
dc.date.accessioned2021-04-08T12:08:27Z
dc.date.available2021-04-08T12:08:27Z
dc.date.issued2016
dc.identifier10.1002/ardp.201600092
dc.identifier.issn03656233
dc.identifier.urihttps://www.scopus.com/inward/record.uri?eid=2-s2.0-85000399323&doi=10.1002%2fardp.201600092&partnerID=40&md5=ee0ffe8aef2265744fac0615a58d52c2
dc.identifier.urihttp://acikerisim.bingol.edu.tr/handle/20.500.12898/4601
dc.description.abstractCarbonic anhydrase (CA, EC 4.2.1.1) is a member of the metalloenzyme family. It catalyzes the rapid conversion of carbon dioxide (CO2) and water to bicarbonate (HCO3 −) and protons (H+) and also plays an important role in biochemical and physiological processes. In this study, a number of novel 2-(4-(aryl)thiazole-2-yl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione derivatives were synthesized and evaluated for their inhibitory characteristics against the human CA isoenzymes I and II (hCA I and hCA II). The structures of the new molecules 8a–i were confirmed by means of IR, 1H NMR, 13C NMR, and elemental analysis. These compounds exhibited excellent inhibitory effects, in the low nanomolar range, with Ki values in the range of 27.07–37.80 nM against hCA I and in the range of 11.80–25.81 nM against hCA II. Our findings suggest that the new isoindolylthiazole derivatives have superior inhibitory effect over acetazolamide (AZA), which is used as clinical CA inhibitor with Ki values of 34.50 and 28.93 nM against the hCA I and hCA II isoenzymes, respectively. © 2016 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
dc.language.isoEnglish
dc.sourceArchiv der Pharmazie
dc.titleSynthesis and Carbonic Anhydrase Inhibition of Novel 2-(4-(Aryl)thiazole-2-yl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione Derivatives


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