Synthesis and biological evaluation of some novel 1-indanone thiazolylhydrazone derivatives as anti-Trypanosoma cruzi agents

被引：43

作者：

Caputto, Maria E. ^{[1
]}

Ciccarelli, Alejandra ^{[2
]}

Frank, Fernanda ^{[3
,4
,5
]}

Moglioni, Albertina G. ^{[1
]}

Moltrasio, Graciela Y. ^{[6
]}

Vega, Daniel ^{[7
,8
]}

Lombardo, Elisa ^{[2
]}

Finkielsztein, Liliana M. ^{[1
]}

机构：

[1] Univ Buenos Aires, Fac Farm & Bioquim, Dept Farmacol, RA-1113 Buenos Aires, DF, Argentina

[2] Hosp Clin Jose San Martin, UBA CONICET, Ctr Invest Porfirinas & Porfirias CIPYP, RA-1120 Buenos Aires, DF, Argentina

[3] Univ Buenos Aires, Fac Farm & Bioquim, CONICET UBA, Catedra Inmunol, RA-1113 Buenos Aires, DF, Argentina

[4] Univ Buenos Aires, Fac Farm & Bioquim, CONICET UBA, Inst Estudios Inmunidad Humoral IDEHU, RA-1113 Buenos Aires, DF, Argentina

[5] Univ Buenos Aires, Fac Med, Dept Microbiol Parasitol & Inmunol, RA-1121 Buenos Aires, DF, Argentina

[6] Univ Buenos Aires, Fac Farm & Bioquim, Dept Quim Organ, RA-1113 Buenos Aires, DF, Argentina

[7] Univ Nacl Gen San Martin, Dept Fis Mat Condensada Gerencia Invest & Aplicac, Comis Nacl Energia Atom, RA-1650 Buenos Aires, DF, Argentina

[8] Univ Nacl Gen San Martin, ECyT, RA-1650 Buenos Aires, DF, Argentina

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2012年 / 55卷

关键词：

Thiazolylhydrazones; Chagas's disease; Anti-Trypanosoma cruzi compounds; Microwave assisted synthesis; SELECTIVE INHIBITORY-ACTIVITY; CHAGAS-DISEASE; 2,4-DISUBSTITUTED THIAZOLES; IN-VITRO; CHEMOTHERAPY;

D O I：

10.1016/j.ejmech.2012.07.013

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel 4-arylthiazolylhydrazones (TZHs) derived from 1-indanones were synthesized in good yields (66-92%) in a simple procedure using microwave irradiation and then characterized by spectroscopy studies. The compounds were evaluated for their in vitro anti-Trypanosoma cruzi activity against the epimastigote, trypomastigote and amastigote forms of the parasite. Most TZHs displayed excellent activity, and were more potent and selective than the reference drug Benznidazole, used in the current chemotherapy. Analysis of the free sterols from parasite incubated with the compounds showed that inhibition of ergosterol biosynthesis is a possible target for the action of these new TZHs. In particular, TZH 9 emerged as a promising antichagasic compound to be evaluated in animal models. (C) 2012 Elsevier Masson SAS. All rights reserved.

引用

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页码：155 / 163

页数：9

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