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- W2554994648 abstract "Carbonic 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, 1 H NMR, 13 C 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." @default.
- W2554994648 created "2016-11-30" @default.
- W2554994648 creator A5002949310 @default.
- W2554994648 creator A5021254018 @default.
- W2554994648 creator A5025673440 @default.
- W2554994648 creator A5040707147 @default.
- W2554994648 creator A5050370140 @default.
- W2554994648 date "2016-11-18" @default.
- W2554994648 modified "2023-10-01" @default.
- W2554994648 title "Synthesis 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" @default.
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- W2554994648 doi "https://doi.org/10.1002/ardp.201600092" @default.
- W2554994648 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/27859585" @default.
- W2554994648 hasPublicationYear "2016" @default.
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