Design and synthesis of novel tetrahydronaphthyl azoles and related cyclohexyl azoles as antileishmanial agents

A novel series of trans-2-aryloxy-1,2,3,4,-tetrahydronaphthyl azoles and related cyclohexyl azoles were synthesized and evaluated in vitro against Leishmania donovani. Compound 9 identified as most active analog with IC50 value of 0.64 μg/mL and SI value of 34.78 against amastigotes, and is several folds more potent than the reference drugs sodium stilbogluconate and paromomycin. It also exhibited significant in vivo inhibition of 83.33%, and provided a new structural scaffold for antileishmanials.

Graphical abstractA novel series of aryloxy tetrahydronaphthyl and cyclohexyl azoles were synthesized as antileishmanials. Among all, compound 9 was identified as the most potent analogue with both in vitro and in vivo activity against Leishmania donovani.Figure optionsDownload full-size imageDownload as PowerPoint slide