Table 1.

Inhibition data of hCA isoforms hCA I, II, IX and XII for sulphonamides using AAZ as standard drug.

Comps	R	R1	KI (nM)a				Selectivity analysis
			hCA I	hCA II	hCA IX	hCA XII	hCA I/IX	hCA I/XII	hCA II/IX	hCA II/XII
1	–	–	31.5	0.62	–	0.59	–	53.12	–	1.05
2	COPh	H	592.7	140.8	40.7	13.0	15	46	3.5	11
3	CO(4-Br-Ph)	H	1447	174.7	75.2	69.6	19	21	2.3	2.5
4	CO(4-Cl-Ph)	H	758.7	186.6	8.0	10.8	95	70	23	17
5	CO(4-F-Ph)	H	399.5	95.4	16.5	9.1	24	44	5.8	10
6	CO(4-CH3-Ph)	H	471.0	116.2	25.1	85.1	19	5.5	4.6	1.4
7	CO(4-Br-Ph)	CH3	978.3	202.6	63.2	76.8	15	13	3.2	2.6
8	CONH2	H	114.5	25.4	34.5	2.4	3.3	48	0.7	11
9	CONHPh	H	459.7	69.7	27.3	38.4	17	12	2.6	1.8
10	CONH(4-Br-Ph)	H	697.1	119.3	64.9	61.0	11	11	1.8	2
11	CONH(4-Cl-Ph)	H	726.4	92.0	66.8	31.6	11	23	1.4	2.9
12	CONH(4-F-Ph)	H	548.6	87.6	12.7	8.7	43	63	6.9	10
13	CONH(4-CH3-Ph)	H	878.1	304.6	37.4	45.2	23	19	8.1	6.7
14	CONH(4-OCH3-Ph)	H	2567	266.1	84.0	49.1	31	52	3.2	5.4
15	CONH(4-OC2H5-Ph)	H	3654	684.2	35.9	59.7	102	61	19	11
16	CONH(4-COCH3-Ph)	H	1697	200.1	24.1	22.5	70	75	8.3	8.9
17	CONH(3,4,5-tri-OCH3-Ph)	H	2672	519.4	100.4	16.9	27	158	5.2	31
18	CONH(4-F-Bn)	H	2048	975.4	256.4	113.4	8	18	3.8	8.6
19	CONH(3,4-diOCH3-Bn)	H	5467	1099	145.1	97.3	38	56	7.6	11
20	CONH(4-Cl-Ph)	CH3	3628	75.4	18.6	66.7	195	54	4.1	1.1
AAZ	–		250.0	12.0	25.0	5.7	10	44	0.5	2.1

^aMean from 3 different assays, obtained using a stopped flow technique (errors were in the range of ±5–10% of the reported values).