Table 3 Comparative inhibition data of selected, potential anion inhibitors of rSmCA

From: Crystal structure and chemical inhibition of essential schistosome host-interactive virulence factor carbonic anhydrase SmCA

Ki [mM]

Compound

hCA I

hCA II

SmCA

F−

>300

>300

6.44

Cl−

6

200

9.45

Br−

4

63

9.35

I−

0.3

26

5.11

CNO−

0.0007

0.03

4.18

SCN−

0.2

1.60

3.15

CN−

0.0005

0.02

2.05

N3−

0.0012

1.51

2.43

HCO3−

12

85

5.10

CO3−

15

73

8.86

NO3−

7

35

7.87

NO2−

8.4

63

5.56

HS−

0.0006

0.04

5.96

HSO3−

18

89

>100

SnO32−

0.57

0.83

4.11

SeO42−

118

112

6.33

TeO42−

0.66

0.92

>100

OsO52−

0.92

0.95

7.55

P2O74−

25.77

48.50

>100

V2O74−

0.54

0.57

4.10

B4O72−

0.64

0.95

8.00

ReO4−

0.11

0.75

8.75

RuO4−

0.101

0.69

2.07

S2O82−

0.107

0.084

7.85

SeCN−

0.085

0.086

2.16

CS32−

0.0087

0.0088

6.16

Et2NCS2−

0.0008

0.0031

0.59

CF3SO3−

nt

nt

5.62

SO42−

63

>200

6.86

ClO4−

>200

>200

>100

BF4−

>200

>200

>100

FSO3−

0.79

0.46

6.02

NH(SO3)2−

0.31

0.76

7.59

H2SO3H

0.021

0.39

0.017

H 2 NSO 2 NH 2

0.31

1.13

0.007

Ph-B(OH) 2

58.6

23.1

0.020

Ph-AsO 3 H 2

31.7

49.2

0.029

  1. Ki values obtained using the stopped-flow CO2 hydrase assay; data for recombinant human isoforms hCAI and hCAII from64. Errors are in the range of 3–5% of the reported data (from three different assays); bold text indicates the three compounds (sulfamide, phenylboronic acid, and phenylarsonic acid) with highest relative affinity for SmCA v the human isoforms
  2. nt  not tested
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