Synthesis and activity of benzopiperidine, benzopyridine and phenyl piperazine based compounds against Leishmania infantum

Abstract

In the present study, anti-leishmanial evaluation of twenty four structurally diverse compounds based on benzopiperidine, benzopyridine and phenylpiperazine nucleuses against Leishmania infantum has been reported. Cytotoxicity studies of all the compounds were performed on murine non-infected splenocytes. Tested compounds exhibited weak to potent activity against promastigote (IC₅₀ 3.21 ± 1.40 to >100 μM) as well as amastigote (IC₅₀ 6.84 ± 2.5 to 92.47 ± 17.61 μM) forms of tested strains. Moreover, two compounds F13 and F15 exhibited potent activity (IC₅₀ < 10 μM) against both forms of the parasite with selectivity index ranges from 11.40 to 22.10. Overall, the current study afforded few hits with novel anti-leishmanial activity in low micromolar concentration, further hit optimization studies can be performed to get more potent candidates against the selected species of parasite.

Keywords: Amphotericin B; Cytotoxicity; Schiff base; Splenocytes; Tetrahydroisoquinoline; Tetrahydroquinoline.