title: Novel Agents against Miltefosine-Unresponsive Leishmania donovani.
abstract: Visceral leishmaniasis is a deadly endemic disease. Unresponsiveness to the only available oral drug miltefosine poses a big challenge for the chemotherapy of the disease. We report a novel molecule, PS-203 {4-(4,4,8-trimethyl-7-oxo-3-oxabicyclo[3.3.1]non-2-yl)-benzoic acid methyl ester}, as effective against a miltefosine-unresponsive strain of the parasite. Further, combinations of PS-203 with miltefosine were also evaluated and showed promising results against a miltefosine-unresponsive strain.
authors.affiliation: Department of Biosciences and Bioengineering, Indian Institute of Technology Guwahati, Assam, India.
authors.forename: Mousumi
authors.initials: M
authors.lastname: Das
authors.affiliation: Department of Biosciences and Bioengineering, Indian Institute of Technology Guwahati, Assam, India.
authors.forename: Gundappa
authors.initials: G
authors.lastname: Saha
authors.affiliation: Department of Chemistry, Indian Institute of Technology Guwahati, Assam, India.
authors.forename: Anil K
authors.initials: AK
authors.lastname: Saikia
authors.affiliation: Department of Biosciences and Bioengineering, Indian Institute of Technology Guwahati, Assam, India vdubey@iitg.ernet.in.
authors.forename: Vikash Kumar
authors.initials: VK
authors.lastname: Dubey
mesh_terms: D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D001565:Benzoates / Q000138:chemical synthesis / Q000494:pharmacology*; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000138:chemical synthesis / Q000494:pharmacology*; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004351:Drug Resistance / Q000187:drug effects*; D004357:Drug Synergism; D006801:Humans; D007893:Leishmania donovani / Q000187:drug effects* / Q000254:growth & development; D008264:Macrophages / Q000187:drug effects / Q000469:parasitology; D021261:Parasitic Sensitivity Tests; D010767:Phosphorylcholine / Q000031:analogs & derivatives / Q000494:pharmacology
chemical_list: C000610408:4-(4,4,8-trimethyl-7-oxo-3-oxabicyclo(3.3.1)non-2-yl)benzoic acid methyl ester; D000981:Antiprotozoal Agents; D001565:Benzoates; D019086:Bridged Bicyclo Compounds, Heterocyclic; D010767:Phosphorylcholine; C039128:miltefosine