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Issue 3, 2010
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Development of second generation amidinohydrazones, thio- and semicarbazones as Trypanosoma cruzi-inhibitors bearing benzofuroxan and benzimidazole 1,3-dioxide core scaffolds

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Abstract

Trypanosoma cruzi is the causative agent of Chagas' disease. The thiosemicarbazone moiety as a pharmacophore has been described for inhibition of the essential cysteine protease, cruzipain, of this parasite. Our recent study identified an amidinohydrazone containing benzofuroxan as a hit compound for cruzipain inhibition with trypanosomicidal activity. Structural modification of the amidinohydrazone, thio- and semicarbazone motifs, using benzofuroxan and including a benzimidazole 1,3-dioxide system as new core scaffolds are described. These changes allowed for the identification of new structural motifs with desired antitrypanosomal activity. The new amidinohydrazone, thio-, and semicarbazone derivatives had excellent anti-trypanosomal activity without improved cruzipain-inhibitory activity compared with the parent compounds. Relevant structural features of these derivatives for further modification have also been determined.

Graphical abstract: Development of second generation amidinohydrazones, thio- and semicarbazones as Trypanosoma cruzi-inhibitors bearing benzofuroxan and benzimidazole 1,3-dioxide core scaffolds

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Article information


Submitted
19 Jun 2010
Accepted
19 Jul 2010
First published
11 Aug 2010

Med. Chem. Commun., 2010,1, 216-228
Article type
Concise Article

Development of second generation amidinohydrazones, thio- and semicarbazones as Trypanosoma cruzi-inhibitors bearing benzofuroxan and benzimidazole 1,3-dioxide core scaffolds

A. Merlino, D. Benitez, S. Chavez, J. Da Cunha, P. Hernández, L. W. Tinoco, N. E. Campillo, J. A. Páez, H. Cerecetto and M. González, Med. Chem. Commun., 2010, 1, 216
DOI: 10.1039/C0MD00085J

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