title: Synthesis and anti-leishmanial activity of 1-aryl-β-carboline derivatives against Leishmania donovani.
abstract: β-carbolines from various natural and synthetic sources have been known to show diverse biological activities. As a part of our current ongoing project to search for potent natural product-derived anti-leishmanial compounds, we have synthesized a series of substituted 1-aryl-β-carboline derivatives. A total of 22 compounds were synthesized and tested in vitro against Leishmania donovani, out of which 6 compounds (4, 5, 10, 11, 19 and 22) showed notably more activity than the standard miltefosine (IC(50) 12.07±0.82 μM), with compound 4 being the most potent (IC(50) 2.16±0.26 μM).
authors.affiliation: Department of Natural Products, National Institute of Pharmaceutical Education and Research (NIPER), Sector 67, S.A.S. Nagar, Punjab 160062, India.
authors.forename: Vikrantsinh M
authors.initials: VM
authors.lastname: Gohil
authors.forename: Keyur G
authors.initials: KG
authors.lastname: Brahmbhatt
authors.forename: Philippe M
authors.initials: PM
authors.lastname: Loiseau
authors.forename: Kamlesh K
authors.initials: KK
authors.lastname: Bhutani
mesh_terms: D002243:Carbolines / Q000138:chemical synthesis* / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D007893:Leishmania donovani / Q000187:drug effects* / Q000254:growth & development; D010767:Phosphorylcholine / Q000031:analogs & derivatives / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D002243:Carbolines; D014344:Trypanocidal Agents; D010767:Phosphorylcholine; C039128:miltefosine