Investigation of the effect of structure modification of furamidine on the DNA minor groove binding and antiprotozoal activity

卷:252

Article

关键词: DRUG-RESISTANCE;    ANALOGS;    ARYLIMIDAMIDES;    RECOGNITION;    EFFICACY;    INDOLE;   

DOI  :  10.1016/j.ejmech.2023.115287

来源: SCIE

【 摘 要 】

New analogs of the antiprotozoal agent Furamidine were prepared utilizing Stille coupling reactions and ami-dation of the bisnitrile intermediate using lithium bis-trimethylsilylamide. Both the phenyl groups and the furan moiety of furamidine were replaced by heterocycles including thiophene, selenophene, indole or benzimidazole. Based upon the Delta Tm and the CD results, the new compounds showed strong binding to the DNA minor groove. The new analogues are also more active both in vitro and in vivo than furamidine. Compounds 7a, 7b, and 7f showed the highest activity in vivo by curing 75% of animals, and this merits further evaluation.

【 授权许可】

Free