Bistacrines as potential antitrypanosomal agents

Ines Schmidt; Sarah G?llner; Antje Fu?August StichAnna KucharskiTanja SchirmeisterElena KatzowitschHeike BruhnAlexandra MiliuR. Luise Krauth-SiegelUlrike Holzgrabe

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Bistacrines as potential antitrypanosomal agents

机译：Bistacrines as potential antitrypanosomal agents

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Graphical abstract Display Omitted Abstract Human African Trypanosomiasis (HAT) is caused by two subspecies of the genus Trypanosoma , namely Trypanosoma brucei rhodesiense and Trypanosoma brucei gambiense . The disease is fatal if left untreated and therapy is limited due to only five non-adequate drugs currently available. In preliminary studies, dimeric tacrine derivatives were found to inhibit parasite growth with IC 50 -values in the nanomolar concentration range. This prompted the synthesis of a small, but smart library of monomeric and dimeric tacrine-type compounds and their evaluation of antiprotozoal activity. Rhodesain, a lysosomal cathepsin-L like cysteine protease of T. brucei rhodesiense is essential for parasite survival and likely target of the tacrine derivatives. In addition, the inhibition of trypanothione reductase by bistacrines was found. This flavoprotein oxidoreductase is the main defense against oxidative stress in the thiol redox system unique for protozoa. >

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《Bioorganic and medicinal chemistry》 |2017年第16期|4526-4531|共6页
作者
Ines Schmidt; Sarah G?llner; Antje Fu?August StichAnna KucharskiTanja SchirmeisterElena KatzowitschHeike BruhnAlexandra MiliuR. Luise Krauth-SiegelUlrike Holzgrabe;
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作者单位

Biochemistry Center (BZH), Heidelberg University;

Medical Mission Institute;

Institute for Molecular Infection Biology, Julius-Maximilians-University of WürzburgInstitute for Pharmacy and Food Chemistry, Julius-Maximilians-University of WürzburgInstitute for Pharmacy and Biochemistry, Johannes-Gutenberg-University of Mainz;

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正文语种英语
中图分类药学;
关键词
Bistacrine; Antitrypanosomal drugs; Rhodesain; Trypanothione reductase;

Bistacrines as potential antitrypanosomal agents

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