Table 1.

Inhibition data of CA I and CA II with compounds reported here and the standard sulphonamide inhibitor acetazolamide (ACTZ) by a stopped-flow CO₂ hydrase assay.

Code	R	R1	Ki (nM)a
			hCA I	hCA II
1	–H	–H	28.5	2.2
2	–CH(CH3)2	–H	>10,000	>10,000
3	–CH2–CH2–C6H5	–H	7352.3	>9641.0
4	–CH3	–CH3	>10,000	9062.9
5	–C2H5	–C2H5	>10,000	>10,000
6	–C6H5	–C6H5	>10,000	>10,000
7	–(CH2)5–		>10,000	>10,000
8	–(CH2)2–N(-CH3)–(CH2)2–		>10,000	>10,000
9	–H	–	>10,000	>10,000
10	2–OH	–	5515.8	8873.4
11	3–OCH3	–	>10,000	>10,000
12	4–OCH3	–	>10,000	>10,000
13	2–Cl	–	>10,000	>10,000
14	3–Cl	–	>10,000	>10,000
15	4–Cl	–	7497.8	>10,000
16	2–CH3	–	>10,000	>10,000
17	3–CH3	–	>10,000	>10,000
18	4–CH3	–	>10,000	>10,000
19	4–C2H5	–	>10,000	>10,000
20	3–NO2	–	>10,000	>10,000
21	4–NO2	–	>10,000	>10,000
22	4–COOH	–	>10,000	>10,000
ACTZ	–	–	250	12

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