Table 2 SAR Studies of naphthalene ring region

From: Design, synthesis and optimization of TarO inhibitors as multifunctional antibiotics against Methicillin-resistant Staphylococcus aureus

Compounds

R3

IC50 (μg/mL)a,b

clogPc

8

n.a.

7.4

9

3.48

5.3

10

0.07

7.1

11

1.00

6.5

12

2.60

6.2

13

n.a.

5.8

14

2.08

5.9

15

n.a.

6.3

16

n.a.

4.1

17a

2.09

4.5

18a

1.88

3.2

19

n.a.

3.6

20

n.a.

4.6

21

n.a.

4.6

22

n.a.

4.5

23

4.00

6.4

24

n.a.

6.0

25

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n.a.

6.9

26

n.a.

6.6

27

n.a.

6.3

  1. aIC50 is calculated based on the relative inhibition rate of compounds against the wild-type strain at different concentrations, dose–response curve was shown in Fig. 4 and Supplementary Fig. 2.
  2. bn.a. means that IC50 cannot be calculated and given from the response curve within the test range.
  3. cclogP data were calculated by software Chemdraw.
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