title: Synthesis and biological evaluation of chalcones as potential antileishmanial agents.
abstract: Antileishmanial activities of thirty-five synthetic chalcones have been examined. Among them, ten compounds (4, 6, 16, 22, 23, 24, 25, 29, 35 and 37) exhibited potent in vitro activity (IC50 range from 1.70 to 8 μM) against extracellular promastigotes and intracellular amastigotes form of Leishmania donovani. Two promising compounds 22 and 37 were tested in vivo in L. donovani/hamster model. Chalcone 37 showed 83.32% parasite inhibition at a dose of 50 mg/kg for 10 days whereas, 75.89% parasite inhibition at 100 mg/kg dose for 5 days by intraperitoneal route at day 7 post-treatment.
authors.affiliation: Division of Medicinal and Process Chemistry, CSIR-Central Drug Research Institute, Lucknow 226 031, India.
authors.forename: Shweta
authors.initials: S
authors.lastname: Gupta
authors.affiliation: Division of Parasitology, CSIR-Central Drug Research Institute, Lucknow 226 031, India.
authors.forename: Rahul
authors.initials: R
authors.lastname: Shivahare
authors.affiliation: Division of Medicinal and Process Chemistry, CSIR-Central Drug Research Institute, Lucknow 226 031, India.
authors.forename: Venkateswarlu
authors.initials: V
authors.lastname: Korthikunta
authors.affiliation: Division of Medicinal and Process Chemistry, CSIR-Central Drug Research Institute, Lucknow 226 031, India.
authors.forename: Rohit
authors.initials: R
authors.lastname: Singh
authors.affiliation: Division of Parasitology, CSIR-Central Drug Research Institute, Lucknow 226 031, India.
authors.forename: Suman
authors.initials: S
authors.lastname: Gupta
authors.affiliation: Division of Medicinal and Process Chemistry, CSIR-Central Drug Research Institute, Lucknow 226 031, India. Electronic address: t_narendra@cdri.res.in.
authors.forename: Narender
authors.initials: N
authors.lastname: Tadigoppula
mesh_terms: D000818:Animals; D002460:Cell Line; D047188:Chalcones / Q000008:administration & dosage / Q000138:chemical synthesis / Q000494:pharmacology*; D002522:Chlorocebus aethiops; D006224:Cricetinae; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D007274:Injections, Intraperitoneal; D007893:Leishmania donovani / Q000187:drug effects*; D007898:Leishmaniasis, Visceral / Q000188:drug therapy* / Q000469:parasitology; D008264:Macrophages / Q000187:drug effects* / Q000469:parasitology; D051379:Mice; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000494:pharmacology*; D014709:Vero Cells
chemical_list: D047188:Chalcones; D014344:Trypanocidal Agents
keywords: Antileishmanial; Chromenochalcones; Chromenodihydrochalcones; Leishmania donovani/hamster model