Synthesis and evaluation of antitrypanosomal activity of some thiosemicarbazide derivatives of 1-butyl-6-fluoro-7-morpholino-4-oxo-1,4-dihydroquinoline-3-carboxylic acid

被引：4

作者：

Pyrih, Andriy ^{[1
]}

Berninger, Michael ^{[2
]}

Gzella, Andrzej ^{[3
]}

Lesyk, Roman ^{[1
]}

Holzgrabe, Ulrike ^{[2
]}

机构：

[1] Danylo Halytsky Lviv Natl Med Univ, Dept Pharmaceut Organ & Bioorgan Chem, Pekarska 69, UA-79010 Lvov, Ukraine

[2] Univ Wurzburg, Inst Pharm & Food Chem, Am Hubland, Germany

[3] Poznan Univ Med Sci, Dept Organ Chem, Poznan, Poland

来源：

SYNTHETIC COMMUNICATIONS | 2018年 / 48卷 / 14期

关键词：

1,2,4-Triazoles; 1; 3; 4-thiadiazoles; antitrypanosomal activity; fluoroquinolones; X-ray analysis; HUMAN AFRICAN TRYPANOSOMIASIS; BRUCEI; RHODESIENSE; GAMBIENSE; AGENTS; DRUGS; ASSAY;

D O I：

10.1080/00397911.2018.1476889

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The synthesis of thiosemicarbazide of 1-butyl-6-fluoro-7-morpholino-4-oxo-1,4-dihydroquinoline-3-carboxylic acid as well as its heterocyclic derivatives - 1,3,4-thiadiazole and 1,2,4-triazole are described; the modification of proper 1,2,4-triazole derivative by maleimides is also presented. Spectral properties of the prepared compounds and X-ray analysis for the selected compounds were studied. For the compounds antitrypanosomal potential and the toxicity were determined. [GRAPHICS] .

引用

页码：1883 / 1891

页数：9

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