Synthesis and in vitro antitrypanosomal activity of novel Nifurtimox analogues

R Pozas, J Carballo, C Castro, J Rubio

Index: Pozas, Rocio; Carballo, Javier; Castro, Clementina; Rubio, Julieta Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 5 p. 1417 - 1421

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Citation Number: 33

Abstract

Eight novel analogues of Nifurtimox, 4-[(5-nitrofurfurylidene) amino]-3-methylthiomorpholine- 1, 1-dioxide, containing alfa–beta unsaturated amides, were synthesized and evaluated for their in vitro activity against Trypanosoma cruzi epimastigotes. Four derivatives bearing a nitro group at the 5-position of the furan ring were the most active in inhibiting culture growth and provoking cell death, showing trypanocidal activity more than threefold the potency of ...