Design, synthesis and biological evaluation of new potent 5-nitrofuryl derivatives as anti-Trypanosoma cruzi agents. Studies of trypanothione binding site of …

…, A Denicola, MJ Gil, V Martínez-Merino

Index: Aguirre, Gabriela; Cabrera, Eliana; Cerecetto, Hugo; Di Maio, Rossanna; Gonzalez, Mercedes; Seoane, Gustavo; Duffaut, Adelina; Denicola, Ana; Gil, Maria J.; Martinez-Merino, Victor European Journal of Medicinal Chemistry, 2004 , vol. 39, # 5 p. 421 - 431

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Citation Number: 59

Abstract

Design, using force-field calculations on the catalytic site of trypanothione reductase from Trypanosoma cruzi, has led to the development of new 5-nitrofuryl derivatives as potential anti-trypanosomal agents. The synthesized compounds were tested in vitro against T. cruzi and more than 75% of the prepared derivatives showed higher activity than nifurtimox. Compounds 5 and 11, hexyl 4-(5-nitrofurfurylidene) carbazate and N-hexyl 3-(5-nitrofuryl) ...