Table 2 Antiviral activity and PA-PB1 inhibition of tetrazole analogs.

From: Exploring Ugi-Azide Four-Component Reaction Products for Broad-Spectrum Influenza Antivirals with a High Genetic Barrier to Drug Resistance

Compounds

% plaque formation at 5 µM

PAC-PB1N ELISA IC50 (µM)

5

16.5 ± 1.2

4.3 ± 0.1

9a

92.9 ± 4.5

N.D.

9b

97.9 ± 5.3

N.D.

9c

101.3 ± 1.8

26.9 ± 4.1

9d

59.3 ± 0.8

N.D.

9e

62.2 ± 4.3

N.D.

9 f

92.2 ± 9.8

>30

9 g

37.4 ± 3.7

N.D.

9 h

56.5 ± 12.3

N.D.

9i

13.4 ± 0.8

13.6 ± 0.9

9j

98.7 ± 8.0

N.D.

9k

29.5 ± 1.0

7.0 ± 0.6

9 l

29.3 ± 1.3

N.D.

9 m

13.8 ± 1.8

15.1 ± 1.2

9n

16.1 ± 1.2

N.D.

9o

19.5 ± 8.8

9.9 ± 0.7

9p

12.3 ± 2.1

N.D.

9q

73.9 ± 8.2

N.D.

9r

45.4 ± 8.6

N.D.

9 s

87.7 ± 0.9

N.D.

9t

73.0 ± 6.5

N.D.

9 u

22.7 ± 2.2

N.D.

12a

1.9 ± 0.3

7.6 ± 1.4

12b

80.6 ± 4.5

37.0 ± 7.0

Nucleozin

0

>30

Oseltamivir

11.1 ± 2.1

>30

  1. The results are the mean ± S.D. from two independent experiments. N.D. = not determined.
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