Journal
MEDCHEMCOMM
Volume 1, Issue 3, Pages 216-228Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c0md00085j
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Funding
- RIDIMEDCHAG network (CYTED)
- UdelaR (Uruguay)
- CSIC (Spain) [2007UY0004]
- REDCLARA-AECID
- PEDECIBA-ANII
- PH PEDECIBA
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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.
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