Synthesis and evaluation of arylamidine derivatives for new antimicrobial and cytotoxic activities



Document title: Synthesis and evaluation of arylamidine derivatives for new antimicrobial and cytotoxic activities
Journal: Anais da Academia Brasileira de Ciencias
Database: PERIÓDICA
System number: 000409003
ISSN: 0001-3765
Authors: 1
2
3
3
3
3
4
1
Institutions: 1Universidade Federal de Pernambuco, Departamento de Ciencias Farmaceuticas, Recife, Pernambuco. Brasil
2Universidade Federal de Pernambuco, Departamento de Biomedicina, Recife, Pernambuco. Brasil
3Universidade Federal de Pernambuco, Departamento de Antibioticos, Recife, Pernambuco. Brasil
4Universidade Federal de Pernambuco, Nucleo de Nutricao, Vitoria de Santo Antao, Pernambuco. Brasil
Year:
Season: Jun
Volumen: 89
Number: 2
Pages: 1051-1058
Country: Brasil
Language: Inglés
Document type: Artículo
Approach: Experimental, aplicado
English abstract A series of arylamidines 3a-j was designed, synthesized and investigated for antimicrobial activity. Structures of the compounds were confirmed by IR, 1H-NMR and 13C-NMR and a 2D spectroscopic study was performed. A preliminary screening of the antimicrobial tests clearly showed that three out of ten arylamidines, viz, 3f, 3g and 3i, were effective against all the gram-negative bacteria: Klebsiella pneumoniae, Pseudomonas aeruginosa and Salmonella enteric; and against the yeast, candida albicans. Further, the Minimum Inhibitory Concentrations (MIC) against the bacteria and yeast were determined. All compounds 3a-d, 3f, 3g, 3i and 3j were also investigated for their low cytotoxic effects on tested cell lines. Compounds 3d and 3f were the most effective derivatives against HL-60 and HEp-2 cells, respectively, with IC50 value (2µg/mL), and low normal cells toxicity
Disciplines: Medicina,
Química
Keyword: Química farmacéutica,
Arilamidinas,
Síntesis química,
Actividad antimicrobiana,
Citotoxicidad
Keyword: Medicine,
Chemistry,
Medicinal chemistry,
Arylamidines,
Chemical synthesis,
Antimicrobial activity,
Cytotoxicity
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