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. Author manuscript; available in PMC: 2013 Oct 11.
Published in final edited form as: J Med Chem. 2012 Sep 26;55(19):8375–8391. doi: 10.1021/jm3007596

Table 1.

Activity of Salicylanilides against T. gondii

graphic file with name nihms410795u2.jpg
Compound R1 R2 R3 R4 R5 R6 R7 MIC50 MIC90
3a OH H Cl H CH3 H H >1 μM >1 μM
3b OH H Cl H Br H H 750-500 nM 1 μM–750 nM
3c OH H Cl H CH2CH3 H H 500-250 nM 750-500 nM
3d OH H Cl H C≡CH H H >1 μM >1 μM
3e OH H Cl H CH=CH2 H H 500-250 nM 1 μM–750 nM
3f OH H Cl H CF3 H H 500-250 nM 500-250 nM
3g OH H Cl H CN H H >1 μM >1 μM
3h OH H Cl H F H H 570-500 nM 1 μM–750 nM
3i OH H Cl H C(CH3)3 H H 16-8 nM 31-16 nM
3j OH H Cl H CF3 H CF3 31-16 nM 250-125 nM
3k OH H H Cl H NO2 H >1 μM >1 μM
3l OH H Cl H CH2Ph H H 1 μM–750 nM 1 μM–750 nM
3m OH H CH3 Cl H NO2 H 500-250 nM 500-250 nM
3n OH H Cl H Cl H Cl 500-250 nM 500-250 nM
3o OH H Cl H F H F >1 μM >1 μM
3p OH H Cl F H Cl H 750-500 nM 750-500 nM
3q OH H Cl OCH3 OCH3 OCH3 H >1 μM >1 μM
3r OH H Cl Cl H H CN 750-500 nM 1 μM–750 nM
3s OH H Cl H CH3 H CH3 >1 μM >1 μM
3t OH H Cl H C≡CH F H >1 μM >1 μM
3u OH H Cl H OCH2CH3 H H >1 μM >1 μM
3v OH H Cl H OCH3 OCH3 H >1 μM >1 μM
3w OH H Cl H OCH(CH3)2 H H >1 μM >1 μM
3x OH H Cl H OCH3 H CH3 >1 μM >1 μM
3y OH H Cl H OPh H H >1 μM >1 μM
3z OH H Cl H OCH(CF3)2 H H >1 μM >1 μM
3aa OH I I H Cl H H >1 μM >1 μM
3ab OH H Cl H OCH2CH2O H >1 μM >1 μM
3ac OH H F H OCH2CH3 H H >1 μM >1 μM
4 OH H Cl Cl H NO2 H 250-200 nM 250-200 nM
5 OH H Cl Cl H NH2 H >1 μM >1 μM
7a PhC(=O)O H Cl Cl H NO2 H 125-61 nM 250-125 nM
7b graphic file with name nihms410795t1.jpg H Cl Cl H NO2 H >1 μM >1 μM
7c graphic file with name nihms410795t2.jpg H Cl Cl H NO2 H >1 μM >1 μM
7d graphic file with name nihms410795t3.jpg H Cl Cl H NO2 H 750-500 nM 1 μM–750 nM
10a CH3O H F H CH3 H H >1 μM >1 μM
10b CH3O H F H OCH3 H H >1 μM >1 μM
14a graphic file with name nihms410795t4.jpg H Cl Cl H NO2 H 31-16 nM 250-125 nM
14b graphic file with name nihms410795t5.jpg H Cl H CF3 H CF3 250-125 nM 250-125 nM