Synthesis, Anti-Toxoplasma gondii and Antimicrobial Activities of 2-hydrazolyl-3-phenyl-5-(4-nitrobenzylidene)-4-thiazolidinone Substituted Derivatives

被引：0

作者：

Aquino, Thiago M. ^{[1
]}

Nascimento, Andre A. P. L. ^{[1
]}

Spacov, Isabel C. G. ^{[1
]}

Carvalho, Cristiane S. ^{[2
]}

Lima, Vania T. ^{[1
]}

Alves, Anselmo Q. ^{[3
]}

Faria, Antonio R. ^{[3
]}

Araujo, Janete M. ^{[1
]}

Lima, Jose G. ^{[3
]}

Alves, Antonio J. ^{[3
]}

Melo, Edesio J. T. ^{[2
]}

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

机构：

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

[2] Univ Estadual Norte Fluminense, Lab Biol Celular, BR-28015620 Rio De Janeiro, Brazil

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

来源：

LATIN AMERICAN JOURNAL OF PHARMACY | 2011年 / 30卷 / 08期

关键词：

Antimicrobial activity; Anti-Toxoplasma gondii activity; 4-thiazolidinone; thiosemicarbazone; IN-VITRO; BIOLOGICAL-ACTIVITY; 4-THIAZOLIDINONES;

D O I：

暂无

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

A novel series of 2-hydrazolyl-3-phenyl-5-(4-nitrobenzylidene)-4-thiazolidinone substituted (3a-p) has been synthesized. The intermediates 2-hydrazolyl-3-phenyl-4-thiazolidinone substituted (2a-p) were prepared by condensation of benzaldehyde 4-phenyl-3-thiosemicarbazone substituted (la-p) with ethyl chloroacetate. Theses intermediates were submitted to reaction with ethyl 2-cyano-3-(4-nitrophenyl)-acetate to give the title compounds. The 4-thiazolidinones were screened for their anti-Toxoplasma gondii, and all derivatives promoted decrease of percentage of infection of Vero cells, with elimination of intracellular tachyzoites. The LD50 ranged around 0.5 mM for the intracellular parasites and were higher than 10 mM for Vero cells. According to results of antimicrobial activity, only two compounds showed significant inhibition against M. luteus, but demonstrated higher values of MIC and MBC when compared with standard drug.

引用

页码：1567 / 1573

页数：7

共 28 条

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