Synthesis and anti-leishmanial evaluation of 1-phenyl-2,3,4,9-tetrahydro-1H-β-carboline derivatives against Leishmania infantum.

Abstract In the present study, antileishmanial activity of sixteen novel series of tetrahydro-β-carboline derivatives against transgenic infrared fluorescent Leishmania infantum strain has been reported. Among these reported analogues, most of the compounds exhibited potent inhibition against both promastigote (IC 50 from 1.99 ± 1.40 to 20.69 ± 0.95 μM) and amastigote (IC 50 from 0.67 ± 0.05 to 4.16 ± 0.008 μM) forms of L. infantum . Moreover, compound 7l, displayed most potent and selective inhibition of parasite amastigote form with IC 50 0.67 ± 0.05 μM, selectivity index >298.5 and was comparable with standard drug amphotericin B. From this study, a new class of tetrahydro-β-carboline derivatives with potent antileishmanial activity was identified and it needs further extensive study to optimize the lead molecules to win the battle against severe and neglected disease leishmaniasis.