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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 1.

SAR of Nitrile Substitutions

Analogue R′ TGRa TGRa Ex Vivo Parasite Killingb
IC50 (μM) Max Resp. (% inh) 2 hr 4 hr 8 hr 16 hr 24 hr 48 hr 72 hr
graphic file with name nihms146895t1.jpg
2,6,10 		2 CN 6.3 − 102 n.e. curling 25%D 40%D 100%D 100%D 100%D
6 CH3 > 50 − 15 n.e. n.e. n.e. n.e. n.e. sluggish 5%D
7 CH2OH 11.2 − 100 n.e. n.e. n.e. n.e. sluggish sluggish 10%D
8 CHO 0.11 − 105 n.e. n.e. n.e. n.e. sluggish 3%D 5%D
9 COOH 0.63 − 95 n.e. n.e. n.e. n.e. n.e. n.e. n.e.
10 CONH2 17.8 − 75 n.e. n.e. 12%D 27%D 60%D 100%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.