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. 2002 Sep 2;12(17):2395-8.
doi: 10.1016/s0960-894x(02)00465-1.

Antileishmanial dinitroaniline sulfonamides with activity against parasite tubulin

Gautam Bhattacharya  1 , Manar M Salem, Karl A Werbovetz
Affiliations

Antileishmanial dinitroaniline sulfonamides with activity against parasite tubulin

Gautam Bhattacharya et al. Bioorg Med Chem Lett. .

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.

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