Enzymatic Assay (EA) and binding constant (Ka) values of thiazole-linked coumarin piperazine hybrids (10a–i).
Compound | % Inhibition (EA) | Gal-1 Ka (104 M−1) | Gal-3 Ka (10−6 M−1) | LdPasea |
---|---|---|---|---|
10a | 58.19 ± 1.12 | 8.8 | NE | NE |
10b | 25.93 ± 0.81 | 2.1 | NE | NE |
10c | 22.46 ± 1.67 | 4.1 | NE | NE |
10d | 56.73 ± 2.13 | 6.6 | NE | NE |
10e | 27.80 ± 0.76 | 6.5 | NE | NE |
10f | 80.57 ± 1.77 | 9.3 | 1.1 | NB |
10g | 58.19 ± 3.28 | 9.8 | 1.0 | NB |
10h | <10 | NE | NE | NE |
10i | <10 | NE | NE | NE |
NE – not evaluated, NB – no binding.