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. Author manuscript; available in PMC: 2011 Dec 1.
Published in final edited form as: Chem Biol Drug Des. 2010 Oct 11;76(6):546–551. doi: 10.1111/j.1747-0285.2010.01035.x

Table 3.

Antimalarial and antileishmanial activities of pyridinium oximes

Entry graphic file with name nihms233745t2.jpg Antimalarial Antileishmanial Cytotoxicity
P. falciparum
 L. donovani Vero cells
D6 Clone W2 Clone
IC50 µg/mL IC50 µg/mL IC90 µg/mL IC50 ng/mL
17 R = CH2CH2CH2Br,
R1 = 4-CONH2, X = Br		 3.7
(S.I. > 1.3)		 4.0
(S.I. > 1.2)		 na na nc
21 R = 5-bromothiophen-2-yl,
R1 = 2-CHNOH, X = Cl		 na na 19 40 nc
24 R = benzothiophen-3-yl,
R1 = 2-CHNOH, X = Cl		 na na 18 40 nc
Chloroquine 0.015 0.12 nt nt nt
Artemisinin 0.010 0.0065 nt nt nt
Pentamidine nt nt 1.2 5 nt
Amphotericin B nt nt 0.2 0.4 nt

IC50, the concentration that affords 50% inhibition of plasmodial / leishmanial growth; IC90, the concentration that affords 90% inhibition of leishmanial growth; na, not active; nt, not tested; nc, Not cytotoxic; S.I., selectivity index = IC50 vero cells/IC50 P. falciparum.