Synthesis and anti-leishmanial evaluation of 1-phenyl-2,3,4,9-tetrahydro-1H-β-carboline derivatives against Leishmania infantum
- Eur J Med Chem. 2016 Nov 10:123:814-821. doi: 10.1016/j.ejmech.2016.08.014.
- 1. Medicinal Chemistry Research Laboratory, Department of Pharmacy, Birla Institute of Technology & Science, Pilani 333031, India.
- 2. Departmento de Ciencias Biomedicas, Facultad de Veterinaria, Universidad de Leon, Leon 24071, Spain.
- 3. Medicinal Chemistry Research Laboratory, Department of Pharmacy, Birla Institute of Technology & Science, Pilani 333031, India. Electronic address: [email protected].
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 (IC50 from 1.99 ± 1.40 to 20.69 ± 0.95 μM) and amastigote (IC50 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 IC50 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.