title: 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 (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.
authors.affiliation: Medicinal Chemistry Research Laboratory, Department of Pharmacy, Birla Institute of Technology & Science, Pilani 333031, India.
authors.forename: Penta
authors.initials: P
authors.lastname: Ashok
authors.affiliation: Medicinal Chemistry Research Laboratory, Department of Pharmacy, Birla Institute of Technology & Science, Pilani 333031, India.
authors.forename: Subhash
authors.initials: S
authors.lastname: Chander
authors.affiliation: Departmento de Ciencias Biomedicas, Facultad de Veterinaria, Universidad de Leon, Leon 24071, Spain.
authors.forename: Ana
authors.initials: A
authors.lastname: Tejería
authors.affiliation: Departmento de Ciencias Biomedicas, Facultad de Veterinaria, Universidad de Leon, Leon 24071, Spain.
authors.forename: Laura
authors.initials: L
authors.lastname: García-Calvo
authors.affiliation: Departmento de Ciencias Biomedicas, Facultad de Veterinaria, Universidad de Leon, Leon 24071, Spain.
authors.forename: Rafael
authors.initials: R
authors.lastname: Balaña-Fouce
authors.affiliation: Medicinal Chemistry Research Laboratory, Department of Pharmacy, Birla Institute of Technology & Science, Pilani 333031, India. Electronic address: murugesan@pilani.bits-pilani.ac.in.
authors.forename: Sankaranarayanan
authors.initials: S
authors.lastname: Murugesan
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002243:Carbolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D060326:Chemistry Techniques, Synthetic; D005260:Female; D020128:Inhibitory Concentration 50; D018314:Leishmania infantum / Q000187:drug effects*; D051379:Mice
chemical_list: D000981:Antiprotozoal Agents; D002243:Carbolines
keywords: Amastigote; Leishmaniasis; Neglected disease; Promastigote; Tetrahydro-β-carboline