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Antileishmanial dinitroaniline sulfonamides with activity against parasite tubulin
Gautam Bhattacharya1, Manar M Salem, Karl A Werbovetz
1Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus 43210, USA.
Bioorganic & Medicinal Chemistry Letters
|August 6, 2002
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.