Synthesis and in vitro antiprotozoal activities of water-soluble, inexpensive phenothiazinium chlorides

被引:17
作者
Lu, Yue-Ting [1 ]
Arai, Chika [2 ]
Ge, Jian-Feng [1 ]
Ren, Wu-Sheng [1 ]
Kaiser, Marcel [3 ]
Wittlin, Sergio [3 ]
Brun, Reto [3 ]
Lu, Jian-Mei [1 ]
Ihara, Masataka [2 ]
机构
[1] Soochow Univ, Key Lab Organ Synth Jiangsu Prov, Suzhou 215123, Peoples R China
[2] Hoshi Univ, Inst Med Chem, Shinagawa Ku, Tokyo 1428501, Japan
[3] Swiss Trop & Publ Hlth Inst, CH-4002 Basel, Switzerland
关键词
Antiprotozoal; Phenothiazinium chlorides; In vitro; Plasmodium falciparum; Trypanosoma cruzi; Leishmania donovani; RHODACYANINE DYES; CHAGAS-DISEASE; PHOTOSENSITIZERS; DERIVATIVES; ANALOGS; CHEMOTHERAPY; ADENOSINE; EFFICACY; MODE; DRUG;
D O I
10.1016/j.dyepig.2010.09.001
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
Tropical diseases are serious infectious diseases caused by protozoan parasites in tropical and subtropical regions Novel effective safe and inexpensive drugs are required to treat the parasites and contribute to the global goal of eradication A series of phenothiazinium chlorides were synthesized and evaluated for in vitro activities against Plasmodium falciparum Trypanosoma cruzi Trypanosoma brucei rhodesiense and Leishmania donovani Notably 3 7-bis(piperidinyl)phenothiazinium chloride showed IC50 of 0 097 mu mol L-1 against T cruzi and 3 7-bis(benzyl(methyl)amino)phenothiazinium chloride exhibited IC50 of 0 081 mu mol L-1 against L donovani although the cytotoxicities of these compounds against L-6 cells were observed at low concentration (C) 2010 Elsevier Ltd All rights reserved
引用
收藏
页码:44 / 48
页数:5
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