title: Antileishmanial dinitroaniline sulfonamides with activity against parasite tubulin.
abstract: Novel dinitroaniline sulfonamides based on the herbicide oryzalin 3 were synthesized and evaluated for activity against the parasitic protozoan Leishmania donovani and against leishmanial tubulin, the putative antiparasitic target of oryzalin. A subset of these compounds possess more activity against both Leishmania and the target protein in vitro. Compound 20 displays improved potency against leishmanial tubulin and is 13.4-fold more active against L. donovani axenic amastigotes than oryzalin.
authors.affiliation: Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus 43210, USA.
authors.forename: Gautam
authors.initials: G
authors.lastname: Bhattacharya
authors.forename: Manar M
authors.initials: MM
authors.lastname: Salem
authors.forename: Karl A
authors.initials: KA
authors.lastname: Werbovetz
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004136:Dinitrobenzenes; D020128:Inhibitory Concentration 50; D007893:Leishmania donovani / Q000187:drug effects*; D013329:Structure-Activity Relationship; D013424:Sulfanilamides; D013425:Sulfanilic Acids / Q000138:chemical synthesis / Q000494:pharmacology; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology; D014404:Tubulin / Q000187:drug effects*
chemical_list: D000981:Antiprotozoal Agents; D004136:Dinitrobenzenes; D013424:Sulfanilamides; D013425:Sulfanilic Acids; D013449:Sulfonamides; D014404:Tubulin; C012465:oryzalin