Synthesis, antibacterial and antiproliferative potential of some new 1-pyridinecarbonyl-4-substituted thiosemicarbazide derivatives

被引:0
作者
Monika Pitucha
Maciej Woś
Malgorzata Miazga-Karska
Katarzyna Klimek
Barbara Mirosław
Anna Pachuta-Stec
Agata Gładysz
Grazyna Ginalska
机构
[1] Medical University,Department of Organic Chemistry
[2] Medical University,Chair and Department of Biochemistry and Biotechnology
[3] Maria Curie-Sklodowska University,Department of Crystallography, Faculty of Chemistry
[4] Medical University of Lublin,Department of Medicinal Chemistry
来源
Medicinal Chemistry Research | 2016年 / 25卷
关键词
Thiosemicarbazide; Antibacterial activity; Cytotoxicity; Cell proliferation;
D O I
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中图分类号
学科分类号
摘要
In this study, the antibacterial, cytotoxic and antiproliferative activities of novel thiosemicarbazide derivatives were assessed. Our results demonstrated that some of the novel compounds possess good antibacterial properties against Staphylococcus epidermidis, Streptococcus mutans and Streptococcussanguinis and are only slightly cytotoxic; thus, they exhibit an excellent therapeutic index, which is higher than that of ethacridine lactate. Moreover, our data showed that compounds 2 and 4 have an antiproliferative activity against human breast adenocarcinoma and human hepatocellular carcinoma cell lines. We expect that the novel thiosemicarbazide derivatives can be used as agents for treatment of dental caries and also for chemotherapy support.
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页码:1666 / 1677
页数:11
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[1]  
Alagarsamy V(2010)Synthesis and antibacterial activity of some novel 1-(4-oxo-3-(3- methoxyphenyl)-3H-quinazolin-2-yl)-4-(substituted) thiosemicarbazides AntiInfect Agents Med Chem 10 105-110
[2]  
Kumar BA(2014)Anticancer activities of thiosemicarbazides/thiosemicarbazones: a review Int J Pharm Pharm Sci 6 34-41
[3]  
Parthiban P(2008)The role of Oper Den 33 710-30
[4]  
Sheorey RV(1999) in caries prevention Br J Clin Pharmacol 47 23-776
[5]  
Solomon VR(2008)The therapeutic monitoring of antimicrobial agents Chem Biodivers 5 764-38
[6]  
Arora S(1995)Synthesis and biological evaluation of novel 4-substituted 1-{[4-(10,15,20-triphenylporphyrin-5-yl)phenyl] methylidene}thiosemicarbazides as new class of potential antiprotozoal agents Acta Crystallogr Sect A 51 33-8
[7]  
Agarwal S(2014)An empirical correction for absorption anisotropy BMC Immunol 15 1-3909
[8]  
Singhal S(1985)Streptococcus sanguinis-induced cytokine and matrix metalloproteinase-1 release from platelets J Am Chem Soc 107 3902-341
[9]  
Autio-Gold J(2009)The development and use of quantum mechanical molecular models. 76. AMI: a new general purpose quantum mechanical molecular model J Appl Cryst 42 339-1218
[10]  
Begg JE(2009)A complete structure solution, refinement and analysis program J Med Chem 52 1214-65