Synthesis and biological activity of novel thiourea derivatives as carbonic anhydrase inhibitors

Figures & data

Figure 1. Synthesis of compounds 5a–c.

Figure 2. Synthesis of compounds 9b–e.

Table 1. hCAs I and II inhibition data with studied compounds, phenol and acetazolamide, by an esterase assay with 4-nitrophenylacetate as substrate.

	KI (μM)*
Inhibitor	hCA I	hCA II
Phenol	10.2†	5.50†
5a	3.4	8.7
5b	4.3	14.3
5c	7.6	22.1
9b	73.6	44.2
9c	62.3	26.5
9d	46.1	12.9
AZA	36.2‡	0.37‡

*Mean from at least three determinations. Errors in the range of ∼3% of the reported value (data not shown).

†From Ref. 7.

‡From Ref. 23.