Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.

Rubén Martín-Escolano,Clotilde Marín,Manuel Vega,Álvaro Martin-Montes,Encarnación Medina-Carmona,Carlos López,Carmen Rotger,Antonio Costa,Manuel Sánchez-Moreno

Bioorganic & Medicinal Chemistry（2019）

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摘要

•Improved in vitro efficiency and lower toxicity than Benznidazole.•Activity against different T. cruzi strains, included those Benznidazole-resistant.•Compound 7 obtained promising results in acute and chronic phase treatments.•Compound 7 trypanocidal effect is due to a mitochondrial membrane depolarisation.•Compound 7 should be implemented in future clinical experiments.

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CD,BZN,NFX,MILT,Fe- SOD,ppm,DMSO,DTU,IC,BTs,pi,CP,IS,PCR,ELISA,1H NMR,Rho,AO,SI,IgG,PEP,PK,PPDK,TCA

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