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
收藏
页码：1883 / 1891
页数：9
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