Synthesis of aminocyanopyrazoles via a multi-component reaction and anti-carbonic anhydrase inhibitory activity of their sulfamide derivatives against cytosolic and transmembrane isoforms

Figures & data

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Table 1.  hCA I, II, IX and XII I nhibition data with compounds 1a–1c and 4.

Compound	Ki (µM)*
	hCA I	hCA II	hCA IX	hCA XII
4a	12.6	6.21	0.34	0.49
4b	10.1	7.14	0.29	0.36
4c	9.4	5.37	0.27	0.44
4d	5.4	0.79	1.24	3.12
4e	5.9	1.13	0.75	0.49
4f	3.1	0.82	0.47	0.15
1a	0.12	0.064	0.022	0.008
1b	0.09	0.051	0.011	0.012
1c	0.08	0.024	0.010	0.010

^aMean from 3 different assays by a CO₂ hydrase, stopped flow assay⁴¹.

Scheme 3.  Preparation of sulfamides 8a–c.

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short-legendFigure 3. 

Khalifah RJ. The carbon dioxide hydration activity of carbonic anhydrase. I. Stop-flow kinetic studies on the native human isoenzymes B and C. J Biol Chem 1971, 246:2561–2573.

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