Table 3 Permeability and transporter activity for compounds 4 and 5

From: Potent Rifampicin derivatives can clear MRSA infections at single low doses when concomitantly dosed with Vancomycin

Compound Number

Mean Papp A-B (10−6 cm/s)

Mean Papp B-A (10−6 cm/s)

Mean (B-A/A-B) Efflux Ratio

Mean A-B % Recovery

Mean B-A % Recovery

Caco-2: endogenous transporters

4

2.59

10.3

3.97

52.70%

66.30%

5

1.17

2.92

2.49

16.30%

58.30%

Rifabutin

11

7.15

0.648

64.80%

59.10%

Rifampicin

0.589

5.93

10.1

79.50%

80.80%

MDCK-MDR1: overexpression of Pgp

4

1.38

18.9

13.7

89.10%

54.80%

5

1.33

10.4

7.8

48.20%

46.30%

Rifabutin

3.57

16.8

4.7

91.30%

67.90%

Rifampicin

0.287

6.25

21.8

76.50%

74.40%

Back to article page