Synthesis and evaluation of anti-Toxoplasma gondii and antimicrobial activities of thiosemicarbazides, 4-thiazolidinones and 1,3,4-thiadiazoles

被引：100

作者：

Liesen, Andre P. ^{[1
]}

de Aquino, Thiago M. ^{[1
]}

Carvalho, Cristiane S. ^{[3
]}

Lima, Vania T. ^{[1
]}

de Araujo, Janete M. ^{[1
]}

de Lima, Jose G. ^{[2
]}

de Faria, Antonio R. ^{[2
]}

de Melo, Edesio J. T. ^{[3
]}

Alves, Antonio J. ^{[2
]}

Alves, Elias W. ^{[3
]}

Alves, Anselmo Q. ^{[2
]}

Goes, Alexandre J. S. ^{[1
]}

机构：

[1] Univ Fed Pernambuco, Dept Antibiot, BR-50670901 Recife, PE, Brazil

[2] Univ Fed Pernambuco, Dept Ciencias Farmaceut, BR-50670901 Recife, PE, Brazil

[3] Univ Estadual Norte Fluminense, Lab Biol Celular & Tecidual, BR-28013620 Rio De Janeiro, Brazil

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 45卷 / 09期

关键词：

Imidazole; 1,3,4-Thiadiazole; 4-Thiazolidinone; Antimicrobial activity; Toxoplasma gondii; ANTIPARASITIC DRUG MEGAZOL; CHIH-DFT DETERMINATION; TRYPANOSOMA-CRUZI; DERIVATIVES; THIAZOLIDINONE;

D O I：

10.1016/j.ejmech.2010.05.017

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In this work we reported the synthesis and evaluation of anti-Toxoplasma gondii and antimicrobial activities in vitro of three new compound series obtained from ethyl(5-methyl-1-H-imidazole-4-carboxylate): acylthiosemicarbazide analogues 3a-d, 4-thiazolidinone analogues 4a-d and 1,3,4-thiadiazole analogues 5a-d. All synthesized compounds were characterized by IR, H-1, C-13 NMR and HRMS. The majority of the tested compounds show excellent anti-T gondii activity when compared to hydroxyurea and sulfadiazine. In addition it was also shown that most of the compounds in this study have a better performance against intracellular tachyzoites. The results for antimicrobial activity evaluation showed weak antibacterial and antifungal activities for all the tested molecules, when compared with the standard drugs (chloramphenicol and rifampicin for antibacterial activity; nistatin and ketoconazole for antifungal activity). (C) 2010 Elsevier Masson SAS. All rights reserved.

引用

页码：3685 / 3691

页数：7

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