title: Chemotherapy of leishmaniasis part XIII: design and synthesis of novel heteroretinoid-bisbenzylidine ketone hybrids as antileishmanial agents.
abstract: Some novel heteroretinoid-bisbenzylidine ketone hybrids have been synthesized and evaluated for their in vitro antileishmanial activity against intramacrophagic amastigotes of Leishmania donovani. Among all the nine synthetic compounds, five compounds (7c, 7d and 7f-h) have shown significant (less than 7μM) activity against intramacrophagic amastigotes. The IC50 values of these compounds were found better than the reference drugs sodium stibogluconate (SSG) and miltefosine. This study helped us in identifying the new class of compounds that could be exploited as potent antileishmanial agents.
authors.affiliation: Division of Medicinal and Process Chemistry, CSIR-Central Drug Research Institute, Lucknow 226 031, India.
authors.forename: Avinash
authors.initials: A
authors.lastname: Tiwari
authors.affiliation: Division of Medicinal and Process Chemistry, CSIR-Central Drug Research Institute, Lucknow 226 031, India.
authors.forename: Santosh
authors.initials: S
authors.lastname: Kumar
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: Department of Chemistry, University of Lucknow, Lucknow 226 001, India.
authors.forename: Padam
authors.initials: P
authors.lastname: Kant
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: shivajins@yahoo.co.in.
authors.forename: S N
authors.initials: SN
authors.lastname: Suryawanshi
mesh_terms: D000818:Animals; D000967:Antimony Sodium Gluconate / Q000494:pharmacology; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured; D002522:Chlorocebus aethiops; D020128:Inhibitory Concentration 50; D007659:Ketones / Q000138:chemical synthesis*; D007893:Leishmania donovani / Q000187:drug effects*; D007896:Leishmaniasis / Q000188:drug therapy* / Q000469:parasitology; D008264:Macrophages / Q000187:drug effects / Q000469:parasitology; D051379:Mice; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D010767:Phosphorylcholine / Q000031:analogs & derivatives / Q000494:pharmacology; D012176:Retinoids / Q000737:chemistry*; D013329:Structure-Activity Relationship; D014709:Vero Cells
chemical_list: D000981:Antiprotozoal Agents; D007659:Ketones; D012176:Retinoids; D010767:Phosphorylcholine; C039128:miltefosine; D000967:Antimony Sodium Gluconate
keywords: Bisbenzylidine ketone; Heteroretinoid; In vitro activity; Leishmania donovani