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. Author manuscript; available in PMC: 2012 Aug 11.
Published in final edited form as: J Med Chem. 2011 Jul 18;54(15):5522–5531. doi: 10.1021/jm2005767

Table 2.

Inhibition of Human α-Thrombin by Sulfated Benzofuran Dimers.a

R R′ log IC50 (M) IC50 (μM) ΔY
12a —OCH2CH3 —CH3 −4.22±0.16b 60±22 0.75
12b —OCH3 —CH3 −4.43±0.12 37±11 0.68
12c —OC(CH3)3 —CH3 −5.14±0.18 7.3±3.1 0.84
12d —OCH2 CH2OCH3 —CH3 −3.42±0.13 375±109 0.80
12e —OCH2CH3 —CH2CH3 −3.92±0.05 121±14 0.95
12f —OCH2CH3 —CH(CH3)2 −4.52±0.19 30±13 0.72
13 nac na −3.89±0.20 129±60 0.62
14 N-morpholino —CH3 Incompleted >7100 nac
15 —OH —CH3 −3.43±0.37 ~374e 0.14
17 nac na −3.12±0.35 ~764e 0.95
18 nac na −3.44±0.06 365±57 0.79
19 nac na −4.05±0.26 89±54 0.70
a

Thrombin inhibition was measured in spectrophotometric assay through initial rate of Spectrozyme TH hydrolysis as described in Experimental section.

b

standard error shown is ±1 S.E.

c

Not applicable. See complete structures of 13, 14, 15, 17, 18 and 19 in Figure 2.

d

Full inhibition profile was not measured.

e

The error in IC50 could not be accurately defined because of insufficient number of data points.