The antiplasmodial and antitrypanosomal activities of novel piperazine derivatives of 3-azabicyclo[3.2.2]nonanes

被引：4

作者：

Mohsin, Noor-Ul-Amin ^{[1
]}

Seebacher, Werner ^{[2
]}

Faist, Johanna ^{[2
]}

Hochegger, Patrick ^{[2
]}

Kaiser, Marcel ^{[3
,4
]}

Maser, Pascal ^{[3
,4
]}

Saf, Robert ^{[5
]}

Weis, Robert ^{[2
]}

机构：

[1] Govt Coll Univ Faisalabad, Fac Pharmaceut Sci, Faisalabad, Pakistan

[2] Graz Univ, Inst Pharmaceut Sci, Graz, Austria

[3] Swiss Trop & Publ Hlth Inst, Basel, Switzerland

[4] Univ Basel, Basel, Switzerland

[5] Graz Univ Technol, Inst Chem & Technol Mat ICTM, Graz, Austria

来源：

MONATSHEFTE FUR CHEMIE | 2018年 / 149卷 / 01期

关键词：

Drug research; Hydrogenations; Structure-activity relationships; Amides; Antiprotozoal activity; Bicyclic compounds; HUMAN AFRICAN TRYPANOSOMIASIS; ANTIPROTOZOAL ACTIVITIES; IN-VITRO; BRUCEI; ASSAY; SENSITIVITY; RHODESIENSE; GAMBIENSE; INVITRO; MALARIA;

D O I：

10.1007/s00706-017-2109-3

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Some new piperazine derivatives of antiprotozoal active 3-azabicyclo[3.2.2]nonanes were prepared. Verification of the structures of the new compounds was done by one- and two-dimensional NMR measurements. All new compounds were investigated for their antiplasmodial and antitrypanosomal activities against Plasmodium falciparum NF54 and Trypanosoma brucei rhodesiense. Their cytotoxicity was assessed against L6 cells. Some of the new compounds showed in vitro very good antiplasmodial and excellent antitrypanosomal activities. The most antitrypanosomal active compound was screened in vivo in a mouse model against T. b. rhodesiense. [GRAPHICS]

引用

页码：99 / 109

页数：11

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