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. Author manuscript; available in PMC: 2010 Oct 22.
Published in final edited form as: J Med Chem. 2009 Oct 22;52(20):6474–6483. doi: 10.1021/jm901021k

Table 3.

SAR of Bis Oxadiazole-2-Oxides

Analogue X TGRa TGRa Ex Vivo Parasite Killingb
IC50 (μM) Max Resp. (% inh) 2 hr 4 hr 8 hr 16 hr 24 hr 48 hr
graphic file with name nihms146895t6.jpg
31–35 		2 NA 6.3 − 102 n.e. curling 25%D 40%D 100%D 100%D
31 1,3-Phenyl 3.5 − 95 n.e. curling 45%D 60%D 100%D 100%D
32 1,4-Phenyl 1.0 − 98 n.e. n.e. ND 55%D 82%D 100%D
33 5-Fluoro-1,3 Phenyl 0.48 − 95 n.e. n.e. ND 55%D 78%D 100%D
34 2,5-Thiophene 0.40 − 102 n.e. 8%D ND 62%D 82%D 100%D
35 2,4-Thiophene 0.35 − 92 n.e. 15%D ND 55%D 91%D 100%D
a

data represents the results from three separate experiments.

b

Data collected by visual examination of worm movement and shape. n.e. (no effect) = all worms are scored as active in culture with typical appearance; curling = worms are seen to curl rather than stretch and contract; sluggish = worm movement is significantly reduced; % D = % of worms dead as judged by lack of movement. ND = not determined.