Secondary/tertiary benzenesulfonamides with inhibitory action against the cytosolic human carbonic anhydrase isoforms I and II

Figures & data

Figure 1.  Some clinically used sulfonamides (dorzolamide and dichlorophenamide) or agents in clinical development (indisulam).

Figure 2.  Structures of tested compounds and the standard drug acetazolamide (AZA).

Table 1.  hCA I and CA II inhibition data of the tested and reference compounds.

Compound	KI (μM)
	hCA I	hCA II
1	22.120^a	0.715^a
2	0.419	0.395
3	0.181	0.485
4	0.612	0.290
5	0.386	0.615
6	0.674	0.602
7	0.869	0.381
8	0.501	0.354
9	0.753	0.533
10	0.519	0.734
11	0.482	0.699
12	0.377	0.459
13	6.010	0.779
14	0.339	0.395
15	0.406	0.534
16	0.584	0.639
17	0.316	0.392
18	26.19^a	0.341^a
19	28.38^a	0.276^a
AAZ	0.250	0.012
Indisulam	0.31^b	0.015^b
Dorzolamide	50^b	0.009^b
Dichlorophenamide	1.20^b	0.038^b

*Mean from at least three determinations. Errors in the range of 1–2 % of the reported value (data not shown), ^aFrom ref. 3, ^bFrom ref. 1.

Alp C, Ozsoy S, Alp NA, Erdem D, Gültekin MS, Küfrevioglu OI et al. Sulfapyridine-like benzenesulfonamide derivatives as inhibitors of carbonic anhydrase isoenzymes I, II and VI. J Enzyme Inhib Med Chem 2011; doi:10.3109 /14756366.2011.617745.

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