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. Author manuscript; available in PMC: 2013 Sep 3.
Published in final edited form as: J Med Chem. 2009 Aug 27;52(16):5005–5008. doi: 10.1021/jm9009229

Table 1.

SAR for cruzain inhibitors bearing ester, amide, or heterocyclic linkers.

graphic file with name nihms500828u1.jpg
Compd Linker (L) X C-Ring cruzain IC50 (μM)
1 graphic file with name nihms500828t1.jpg N DiCl-Pha 77
6 CH DiCl-Pha 58
2 N cycloheptyl 87
7 graphic file with name nihms500828t2.jpg N cyclohexyl 16% at 200 μM
8 CH cyclohexyl 15% at 200 μM
9 graphic file with name nihms500828t3.jpg CH cyclohexyl 78
10 CH cycloheptyl 25
11 CH DiMeOPhb 27
a

DiCl-Ph = 2,5-dichlorophenyl,

b

DiMeOPh = 2,4-dimethoxyphenyl