Table 1 SAR of all the targeted compounds for anti-HCV activity in Huh7.5 cells

1

C₆H₄OCH₃-4

COOH

> 1000

43.8 ± 3.81

> 22.8

2

C₆H₄F-4

COOCH₃

274 ± 8.35

2.09 ± 1.65

131

3a

C₆H₄F-4

CH₂OH

285 ± 7.45

2.99 ± 1.51

95.3

3b

CH₂CH₂CH₃

CH₂OH

> 500

16.4 ± 10.9

> 30.5

3c

CH₂(CH₂)₅CH₃

CH₂OH

33.3 ± 6.49

1.01 ± 0.55

32.9

3d

CH₂(CH₂)₆CH₃

CH₂OH

17.8 ± 2.44

0.80 ± 0.26

22.3

6a

C₆H₄OCH₃-4

COOCH₃

414 ± 7.34

7.01 ± 1.51

59.1

6b

C₆H₄CH₃-4

COOCH₃

132.9 ± 7.53

1.73 ± 1.36

76.8

6c

C₆H₄CH = CH₂-4

COOCH₃

81.2 ± 12.9

1.61 ± 0.76

50.4

6d

C₆H₃F₂-2,4

COOCH₃

261 ± 28.7

1.69 ± 1.47

154

6e

C₆H₄NO₂-4

COOCH₃

235 ± 48.2

14.2 ± 3.13

16.5

6f

pyridyl-4

COOCH₃

> 500

4.66 ± 0.35

> 107

7a

C₆H₄OCH₃-4

CH₂OH

383 ± 30.2

2.81 ± 0.82

136

7b

C₆H₄CH₃-4

CH₂OH

252 ± 3.04

< 2.06

> 122

7c

C₆H₄CH = CH₂-4

CH₂OH

143 ± 32.3

3.16 ± 0.51

45.3

7d

C₆H₃F₂-2,4

CH₂OH

266 ± 9.47

< 2.06

> 129

7e

Pyrid-4-yl

CH₂OH

> 500

9.03 ± 5.58

> 55.4

7f

Pyrid-3-yl

CH₂OH

> 500

4.39 ± 3.01

> 114

7 g

pyrid-2-ylCl-5

CH₂OH

> 500

10.9 ± 5.59

> 45.9

7 h

CONHC₆H₄

CH₂OH

> 500

46.7 ± 41.0

> 10.7

7i

CONHC₆H₃CF₃-4

CH₂OH

86.2 ± 4.33

4.19 ± 1.44

20.6

9

41.9 ± 1.10

1.16 ± 0.25

36.1

10a

C₆H₄OCH₃-4

CH₃

> 140 ± 16.6

11.7 ± 0.06

12.0

10b

C₆H₄CH₃-4

CH₃

55.7 ± 7.50

0.82 ± 0.26

67.9

10c

C₆H₄CH₃-4

C₂H₅

12.3 ± 4.23

< 0.23

> 53.5

10d

C₆H₃F₂-2,4

CH₃

156 ± 37.9

6.55 ± 2.69

23.8

10e

Pyrid-4-yl

CH₃

> 500

80.4 ± 24.3

6.22

13a

4-OCH₃

COOCH₃

326 ± 21.0

16.7 ± 4.71

19.5

13b

4-F

COOCH₃

260 ± 84.8

18.1 ± 6.49

14.4

13c

3-NO₂

COOCH₃

402 ± 83.6

40.4 ± 3.64

10.0

14a

4-OCH₃

CH₂OH

214 ± 95.0

8.80 ± 2.15

24.3

14b

4-F

CH₂OH

156 ± 65.8

13.6 ± 2.63

11.5

20

3-NO₂

CH₂OH

312 ± 31.1

18.4 ± 1.64

17.0

Tela

47.6 ± 0.61

0.02 ± 0.02

1950