Bioorganometallic derivatives of 4-hydrazino-benzenesulphonamide as carbonic anhydrase inhibitors: synthesis, characterisation and biological evaluation

Figures & data

Scheme 1. Synthesis of organometallic-hydrazone derivatives 1–3.

Table 1. hCA I, II, IX and XII inhibition data with compounds (1–3)a,b and acetazolamide (AAZ) as standard drug, by a stopped-flow CO2 hydrase assay [25].

KI (nM)^a
	hCA I	hCA II	hCA IX	hCA XII
1a	7.5	22.4	579.8	24.4
2a	5.9	8.2	2.1	3.1
3a	13.2	1.7	49.9	4.9
1b	3.7	9.7	25.0	3.8
2b	268.6	11.2	221.3	3.3
3b	3.6	9.3	41.9	1.9
AAZ	250	12	25.8	5.7

^a Mean from three different assays, by a stopped flow technique (errors were in the range of ± 5–10% of the reported values).

Khalifah RG. 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;246:2561–73.

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