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. Author manuscript; available in PMC: 2013 Sep 1.
Published in final edited form as: Eur J Med Chem. 2012 Jul 14;55:449–454. doi: 10.1016/j.ejmech.2012.06.058

Table 1.

DNA binding, in vitro antileishmanial and cytotoxicity data molecular weight arylimidamides.

code IC50a
L. a. (µM) 		IC50b
L. d. (µM) 		IC50c
Cytotox (µM)		 Δ Tmd
(°C)
DB766 0.087e 0.036e 3.0 6.0
3a >10 NDf >212 0.0
3b ND ND >207 0.0
6 5.1 ND >202 0.5
9a 0.76 0.079 46.9 6.0
9b >10 ND 93.5 2.1
9c 0.67 0.028 5.0 5.2
13 0.14 0.025 22.9 0.1
18 1.1 ND 21.6 4.0
a

IC50 values obtained against intracellular L. a. [14].

b

IC50 values obtained against intracellular L. d. [14].

c

Cytotoxicity (IC50) was evaluated using cultured L6 rat myoblast cells [24,25].

d

Increase in thermal melting of poly(dA-dT)n in °C [21].

e

Values taken from [14].

f

ND, not determined.

Low MW arylimidamides as analogues of DB 766 were prepared

Arylimidamides are synthesized from aryl thioimidates and corresponding diamines

New arylimidamides showed L. d. IC50 values of 25–79 nM and acceptable cytotoxicity

DNA binding affinities and in vivo toxicity reported