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Table 1 Results of biological evaluation

From: Structure–activity relationships in a series of antiplasmodial thieno[2,3-b]pyridines

Code X–a % inhibition ± SD, PfNF54-Luc at 3 µM IC50 [µM], PfNF54-Luc
1 [25] H– n.d. 5.5
2a Cl– 25.7 ± 3.5 6.2
2b F– 28.1 ± 3.3 6.1
2c Br– − 5.9 ± 1.3 n.d.
2d H3C– 12.4 ± 2.4 n.d.
2e HO– 0.2 ± 2.5 n.d.
3a H3CO– 33.2 ± 3.2 12.2
3b H5C2O– 14.5 ± 1.3 n.d.
3c C6H5–CH2–O– 12.8 ± 4.9 n.d.
3d 2-hydroxyethoxy– 25.6 ± 3.3 20.0
3e (2,2-dimethyl-1,3-dioxolan-4-yl)methoxy– − 11.7 ± 0.7 n.d.
3f 2,3-dihydroxypropoxy– 14.7 ± 1.8 n.d.
3g HO2C–CH2–O 31.3 ± 1.1 n.d.
4a Dimethylamino– 29.9 ± 5.6 5.7
(+)4b Diethylamino– 73.0 ± 1.2 1.1
(−)4b Diethylamino– − 24.4 ± 10.4 n.d.
4c Pyrrolidino– 33.0 ± 2.4 n.d.
4d Piperidino– 39.1 ± 1.1 5.0
4e Morpholino– 20.2 ± 4.8 n.d.
4f N-[2-(N-Boc-amino)ethyl)]-N-(methyl)amino– 67.1 ± 2.7 2.5
4g N4-Boc-piperazino– 42.1 ± 2.9 3.8
4h N-(2-dimethylaminoethyl)-N-(methyl)amino– 99.9 ± 0.1 1.2
4i N-(2-aminoethyl)-N-(methyl)amino-(as hydrochloride) 8.1 ± 3.3 n.d.
4j Piperazino-(as hydrochloride) 75.7 ± 1.5 1.5
BS Blasticidin 99.3 ± 0.7 n.d.
  1. n.d. not determined
  2. afor position of X, refer to Fig. 3. All structures are depicted in the Additional file 1