Aryloxy cyclohexyl imidazoles: A novel class of antileishmanial agents

Thirteen novel aryloxy cyclohexane-based mono and bis imidazoles were synthesized and evaluated in vitro as antileishmanials against Leishmania donovani and cytotoxicity assessed. These compounds were better than the existing drugs, sodium stibogluconate and pentamidine in respect to IC50 and SI values. Promising compounds were tested further in vivo. Among all, the bis methylimidazole with 2-fluoro, 4-nitro aryloxy group (9) exhibited significant in vivo inhibition of 77.9%, thus providing new structural lead for antileishmanials.

A series of aryloxy cyclohexane-based mono and bis imidazoles were synthesized and evaluated both in vitro and in vivo against Leishmania donovani. All the 13 compounds displayed very promising in vitro activity while one compound showed significant in vivo activity.Figure optionsDownload as PowerPoint slide