5-Nitro-2-furyl derivative actives against Trypanosoma cruzi: preliminary in vivo studies.
Ten 5-nitro-2-furyl derivatives, with good to excellent in vitro anti-Trypanosoma cruzi activity, and nifurtimox were tested oral and intraperitoneally on healthy animals for its acute toxicity on murine models. According to animals' survival percentage, organ histological results, biochemical and haematological findings, three new derivatives, with toxicity like nifurtimox, were selected to test in vivo as antichagasic agents. Clearly, dependences between chemical structure and both acute toxicity and in vivo anti-T. cruzi activity were observed. 4-Hexyl-1-[3-(5-nitro-2-furyl)-2-propenylidene]semicarbazide displayed good profile as anti-T. cruzi agent and better acute toxicity profile than nifurtimox.
Cabrera
Eliana
E
Departamento de Química Orgánica, Facultad de Química/Facultad de Ciencias, Universidad de la República, Iguá 4225, 11400 Montevideo, Uruguay.
Murguiondo
Mariana González
MG
Arias
Marelina González
MG
Arredondo
Carolina
C
Pintos
Cristina
C
Aguirre
Gabriela
G
Fernández
Marcelo
M
Basmadjián
Yester
Y
Rosa
Raquel
R
Pacheco
José Pedro
JP
Raymondo
Stella
S
Di Maio
Rossanna
R
González
Mercedes
M
Cerecetto
Hugo
H
D000818:Animals; D014355:Chagas Disease / Q000188:drug therapy* / Q000473:pathology; D005260:Female; D051379:Mice; D009547:Nifurtimox / Q000737:chemistry* / Q000627:therapeutic use* / Q000633:toxicity; D009581:Nitrofurans / Q000737:chemistry* / Q000627:therapeutic use* / Q000633:toxicity; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000737:chemistry* / Q000627:therapeutic use* / Q000633:toxicity; D014349:Trypanosoma cruzi / Q000187:drug effects
D009581:Nitrofurans; D014344:Trypanocidal Agents; D009547:Nifurtimox