Abstract
AbstractEleven amino‐substituted 1,4‐naphthoquinones were synthesized via the reaction of 1,4‐naphthoquinone with different primary and secondary mono‐ and diamines in the presence of dichloromethane ethanol (1:2) solvent at room temperature. All compounds were purified by flash column chromatography, characterized by TLC, HPLC, 13C‐NMR, 1H‐NMR, and FT‐IR spectral analysis and were evaluated in vitro for antifilarial activity using adult bovine filarial worm Setaria digitata by assessing worm motility and MTT (3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide) reduction. Seven of the 11 compounds had macrofilaricidal activity with compounds 9 (2‐[(1,3‐dimethylbutyl) amino] naphthalene‐1,4‐dione) and 11 (2‐(4‐methylpiperazin‐1‐yl) naphthalene‐1,4‐dione) having maximum activity (ED50 values of 0.91 and 1.2 µM, respectively, at 48 h). The effect of different substitutions on antifilarial activity is discussed. Drug Dev Res 2009. © 2009 Wiley‐Liss, Inc.
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