Inhibition of the α-carbonic anhydrase from Vibrio cholerae with amides and sulfonamides incorporating imidazole moieties

Figures & data

Scheme 1. General synthesis of 1–9. Reagents and conditions: (a): TEA, dry CH₂Cl₂, 12–48 h, RT.

Scheme 2. Synthesis of 10. Reagents and conditions: (a): TEA, dry CH₂Cl₂, 16 h, RT.

Table 1. Inhibition activity of compounds 1–10 and AAZ against Vibrio cholerae α-carbonic anhydrase, obtained as described in the supplementary information.

		KI (nM)^a
	Compound	hCA I	hCA II	VchCA
1		387.36	>10,000	10.9
2		1697.42	>10,000	8.5
3		>50,000	>50,000	6.4
4		>50,000	>50,000	6.2
5		>50,000	>50,000	39.2
6		>50,000	>50,000	9.1
7		2549.16	>10,000	10.4
8		1730.79	>10,000	11.0
9		>50,000	>50,000	5.4
10		>50,000	>50,000	7.8
AAZ		250	12.1	5.0

^a Data represent the mean of 3 different assays; the mean errors are ±5–10% of the reported values.