Synthesis and characterization of novel dioxoacridine sulfonamide derivatives as new carbonic anhydrase inhibitors

Figures & data

Figure 1.  SDS-PAGE analysis of CA isoenzymes: (a) Standard hCA I, (b) isolated hCA I, (c) standard hCA II, (d) isolated hCA II.

Scheme 1.  Synthesis of acridine-1,3-dion sulfonamides (4–12).

Scheme 2.  New CA inhibitors (4–12).

Table 1.  The K_i values obtained from in vitro inhibition experiments.

Inhibitor	Ki Values (µM)
	hCA I	hCA II
AAZ	3.1–3.0	2.2–2.1
Sulfanilamide	4,6–4,4	3,9–3,8
4	0.38–0.66	0.19–0.31
5	0.08–0.07	0.18–0.12
6	0.05–0.06	0.12–0.14
7	0.01–0.02	0.001–0.002
8	0.008–0.009	0.006–0.008
9	0.13–0.14	0.09–0.10
10	0.04–0.05	0.11–0.14
11	0.19–0.22	0.11–0.13
12	0.21–0.23	0.03–0.04