Synthesis of novel sulfonamides under mild conditions with effective inhibitory activity against the carbonic anhydrase isoforms I and II

Figures & data

Scheme 1. Synthesis of novel sulfonamide derivatives.

Table 1. The effects of synthesized compounds on hCA I and II isozymes under in vitro conditions.

	Hydratase IC50^a^,^b (μM)		Esterase IC50^a^,^b (μM)		Ki^a^,^b (μM)
Compound	hCA I	hCA II	hCA I	hCA II	hCA I	hCA II
AAZ	0.224 ± 0.0042	0.198 ± 0.0071	0.321 ± 0.0051	0.212 ± 0.0048	0.210 ± 0.0035	0.120 ± 0.0049
3	0.741 ± 0.0011	0.312 ± 0.0002	0.276 ± 0.0003	0.237 ± 0.0012	0.149 ± 0.0009	0.141 ± 0.0008
4	0.860 ± 0.0005	0.370 ± 0.0003	0.184 ± 0.0005	0.085 ± 0.0009	0.081 ± 0.0001	0.048 ± 0.0005
6a	1.125 ± 0.0003	0.203 ± 0.0004	0.136 ± 0.0005	0.070 ± 0.0009	0.052 ± 0.0002	0.029 ± 0.0005
6b	1.248 ± 0.0008	0.418 ± 0.0009	0.160 ± 0.0005	0.082 ± 0.0007	0.065 ± 0.0005	0.036 ± 0.0003
6c	0.518 ± 0.0001	0.250 ± 0.0006	0.112 ± 0.0005	0.059 ± 0.0001	0.050 ± 0.0005	0.028 ± 0.0007
6d	0.547 ± 0.0007	0.138 ± 0.0004	0.058 ± 0.0005	0.032 ± 0.0005	0.025 ± 0.0008	0.015 ± 0.0006
6e	0.738 ± 0.0004	0.362 ± 0.0007	0.105 ± 0.0005	0.051 ± 0.0005	0.043 ± 0.0003	0.023 ± 0.0005
6f	0.925 ± 0.0009	0.394 ± 0.0005	0.049 ± 0.0005	0.027 ± 0.0008	0.020 ± 0.0003	0.011 ± 0.0001
6g	1.143 ± 0.0002	0.596 ± 0.0002	0.195 ± 0.0005	0.113 ± 0.0002	0.081 ± 0.0006	0.045 ± 0.0004
6h	1.416 ± 0.0006	0.620 ± 0.0005	0.053 ± 0.0005	0.029 ± 0.0004	0.022 ± 0.0002	0.013 ± 0.0001
6i	1.654 ± 0.0004	1.060 ± 0.0001	0.106 ± 0.0005	0.065 ± 0.0006	0.044 ± 0.0004	0.025 ± 0.0008

AAZ was used as a reference compound.

^aMean ± standard error, from three different assays.

^bp < 0.00001 for all analysis.