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. Author manuscript; available in PMC: 2015 Mar 2.
Published in final edited form as: Eur J Med Chem. 2010 May 20;45(9):3752–3761. doi: 10.1016/j.ejmech.2010.05.024

Table 1.

S. aureus SrtAΔ59 inhibition of synthesized derivatives of inhibitor 1

graphic file with name nihms657730t1.jpg
No X A-B Stereochemistry C D Y R IC50(µM)a
5a S CH=CH E NH O O COOCH3 71 ± 2.5
5b O CH=CH E NH O O COOCH3 58 ± 4.9
6 O CH=CH E NH O O COOH 181 ± 14
7 S CH2-CH2 -b NH O O COOH >600
8 S CH2-CH2 -b NH O O COOCH3 >600
9 O CH2-CH2 -b NH O O COOH >600
10 O CH2-CH2 -b NH O O COOCH3 >600
12 S C≡C -b NH O O COOCH3 165 ± 9
13 S C≡C -b NH O O COOH 183 ± 12
14 S CH=CH Z NH O O COOCH3 61 ± 4
15 S CH=CH Z NH O O COOH 154 ± 5
16a S CH=CH E NMe O O COOCH3 571 ± 43
16b O CH=CH E NMe O O COOCH3 514 ± 39
17a S CH=CH E NMe O O COOH >600
17b O CH=CH E NMe O O COOH >600
19 S CH=CH E NH HH O COOCH3 249 ± 9
20 S CH=CH E NH HH O COOH >600
24a S CH=CH E NH O CH2 COOCH3 92 ± 5
24b O CH=CH E NH O CH2 COOCH3 131 ± 14
25a S CH=CH E NH O CH2 COOH 181 ± 12
25b O CH=CH E NH O CH2 COOH 463 ± 19
26a S CH=CH E NH O O CH2OH 73 ± 2
26b O CH=CH E NH O O CH2OH 111 ± 5.7
27a S CH=CH E NH O O CHO 77 ± 6.5
27b O CH=CH E NH O O CHO 107 ± 8.5
28 S CH=CH E NH O O CONH2 105 ± 3.7
a

IC50 values were determined by a Fluorescent Resonance Energy Transfer (FRET) assay. Reported values are an average of 3–5 measurements.

b

Not applicable