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. Author manuscript; available in PMC: 2012 Oct 1.
Published in final edited form as: Bioorg Med Chem Lett. 2011 Aug 8;21(19):5774–5777. doi: 10.1016/j.bmcl.2011.08.009

Table 3.

Effects of modifications of the sulfur linker on EAAT2 protein levels

graphic file with name nihms322430u4.jpg
Compound X R Fold increase for EAAT2a
4 h 24 h
1 S 2-Cl-6-F-Bn nab 2.0 ± 0.8
8–2 O 2-Cl-6-F-Bn 1.1 ± 0.3 2.9 ± 0.4
7–4 S 2-Me-Bn 1.7 ± 0.1 3.5 ± 0.3
8–1 O 2-Me-Bn 2.0 ± 0.9 2.5 ± 0.5
7–13 S 2,6-di-Me-Bn na 6.5 ± 1.0
8–3 O 2,6-di-Me-Bn 2.1 ± 1.2 3.2 ± 1.4
7–14 S 1-(2-Cl-6-F-phenyl)ethyl 1.7 ± 0.9 5.5 ± 1.0
8–4 O 1-(2-Cl-6-F-phenyl)ethyl 1.6 ± 0.2 3.0 ± 0.7
7–15 S 2-(2-Cl-6-F-phenylethyl) 1.9 ± 0.7 6.7 ± 1.5
8–5 O 2-(2-Cl-6-F-phenylethyl) 2.2 ± 0.4 3.1 ± 1.2
7–16 S 2,4-di-F-Bn 2.4 ± 1.5 3.8 ± 0.8
8–6 O 2,4-di-F-Bn na 2.3 ± 0.6
7–17 S 2,4-di-Me-Bn 1.9 ± 0.8 6.4 ± 1.0
8–7 O 2,4-di-Me-Bn na 2.0 ± 0.9
6–1 S H na 2.0 ± 0.8
5–1 O H 1.5 ± 0.5 1.6 ± 1.0
14 NH 2-Me-Bn 1.7 ± 1.1 2.6 ± 0.5
9–1 SO2 2-Cl-6-F-Bn 1.4 ± 0.3 2.8 ± 0.4
9–2 SO2 2-Me-Bn 2.3 ± 0.4 1.1 ± 0.2
9–3 SO2 2-Cl-Bn 1.6 ± 0.3 na
17–1 CONH n-Pr na 1.2 ± 0.2
17–2 CONH 2-Me-Bn na 1.4 ± 0.2
a

Compound concentration of 10 μM;

b

na = not active