2,5-DIARYL SELENOPHENE COMPOUNDS, AZA 2,5-DIARYL THIOPHENE COMPOUNDS, AND THEIR PRODRUGS AS ANTIPROTOZOAL AGENTS
申请人:Tidwell Richard R.
公开号:US20100331368A1
公开(公告)日:2010-12-30
Novel dicationic 2,5-diaryl selenophene compounds are described. Also described are novel aza analogues of dicationic 2,5-diaryl thiophenes. The presently disclosed dicationic compounds exhibit in vitro activity versus
Trypanosoma brucei rhodesiense, Plasmodium falciparum
, and/or
Leishmania donovani
comparable to that of pentamidine and furamidine. Some of the novel dicationic compounds display good activity in vivo in a murine model of a
Trypanosoma brucei rhodesiense
infection.
本文描述了新型二阳离子2,5-二芳基硒吡咯烷化合物。同时,还描述了新型二阳离子2,5-二芳基噻吩的氮杂环类似物。目前披露的二阳离子化合物在体外对Trypanosoma brucei rhodesiense、Plasmodium falciparum和/或Leishmania donovani表现出与Pentamidine和Furamidine相当的活性。其中一些新型二阳离子化合物在Trypanosoma brucei rhodesiense感染的小鼠模型中表现出良好的体内活性。