Synthesis, characterization and antiglaucoma activity of some novel pyrazole derivatives of 5-amino-1,3,4-thiadiazole-2-sulfonamide.

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Kasimogullari R, Bulbul M, Arslan BS, Gokce B

Synthesis, characterization and antiglaucoma activity of some novel pyrazole derivatives of 5-amino-1,3,4-thiadiazole-2-sulfonamide.

Eur J Med Chem. 2010 Nov;45(11):4769-73. doi: 10.1016/j.ejmech.2010.07.041. Epub 2010 Jul 24.

PubMed ID
20724038 [ View in PubMed
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Abstract

Pyrazole carboxylic acid derivatives of 5-amino-1,3,4-thiadiazole-2-sulfonamide (inhibitor 1) were synthesized from ethyl 3-(chlorocarbonyl)-1-(3-nitrophenyl)-5-phenyl-1H-pyrazole-4-carboxylate compound. The inhibitory effects of inhibitor 1, acetazolamide (AAZ) and of 11 newly synthesized amides (5a-b, 6, 7a-g, and 8) on hydratase and esterase activities of carbonic anhydrase isoenzymes (hCA-I and hCA-II) have been studied in vitro. The comparison of newly synthesized amides to inhibitor 1 and to AAZ indicated that the new derivatives inhibit CA isoenzymes and they are more potent inhibitors than the parent inhibitor 1 and AAZ.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
AcetazolamideCarbonic anhydrase 1Ki (nM)6300N/AN/ADetails
AcetazolamideCarbonic anhydrase 1IC 50 (nM)3800N/AN/ADetails
AcetazolamideCarbonic anhydrase 1IC 50 (nM)3100N/AN/ADetails
AcetazolamideCarbonic anhydrase 2IC 50 (nM)8200N/AN/ADetails
AcetazolamideCarbonic anhydrase 2Ki (nM)3300N/AN/ADetails
AcetazolamideCarbonic anhydrase 2IC 50 (nM)4100N/AN/ADetails