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Journal of Pharmaceutical Negative Results
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ORIGINAL ARTICLE
Year : 2013  |  Volume : 4  |  Issue : 1  |  Page : 19-25

Insignificant level of in vitro cytotoxicity, anti-rotavirus, antibacterial, and antifungal activities of N-alkylmaleamic acids


1 Departamento de Ciências da Saúde, Biológicas e Agrárias, Centro Universitário Norte de Espírito Santo, Universidade Federal do Espírito Santo,Rodovia BR 101 Norte, Km. 60, Bairro Litorâneo, São Mateus, ES, Brazil
2 Departamento de Farmácia and Ciências Biológicas, Universidade Federal de Ouro Preto, Campus Morro do Cruzeiro s/n., Ouro Preto, MG, Brazil
3 Departamento de Farmácia, Universidade Federal de Ouro Preto, Campus Morro do Cruzeiro s/n., Ouro Preto, MG, Brazil
4 Departamento de Ciências Biológicas, Universidade Federal de Ouro Preto, Campus Morro do Cruzeiro s/n., Ouro Preto, MG, Brazil
5 Departamento de Parasitologia, ICB, Universidade Federal de Minas Gerais, Avenida Antônio Carlos, Pampulha, Belo Horizonte, MG, Brazil
6 Departamento de Química, Biotecnologia e Engenharia de Bioprocessos, Universidade Federal de São João Del Rei, Campus Alto Paraopeba, Ouro Branco, MG, Brazil

Correspondence Address:
S.A. Vieira Filho
Departamento de Farmácia, Universidade Federal de Ouro Preto, Campus Morro do Cruzeiro s/n. CEP 35400-000. Ouro Preto, MG
Brazil
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Source of Support: None, Conflict of Interest: None


DOI: 10.4103/0976-9234.116762

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By reacting maleic anhydride with amines, we synthesized the derivatives N-ethyl, N-(2-ethylamine), N-piperidinyl, N-phenyl, and N-phenylhydrazinyl maleamic acids. The purity of these products was initially verified by melting range and the presence of only one spot observed by thin layer chromatography. The chemical structures of the obtained N-alkyl maleamic acids were confirmed through infrared (IR) and hydrogen and carbon nuclear magnetic resonance ( 1 H and 13 C NMR) spectrometry. Due to the already proven pharmacological activity of maleimides, maleic anhydride and its N-alkyl maleamic acids were subjected to in vitro assays to observe antiviral (SA-11 rotavirus), antibacterial (Escherichia coli, Staphylococcus aureus, and Bacillus cereus), antifungal (Colletotrichum musae, Fusarium solani f. sp. phaseoli, Fusarium solani f. sp. piperis Alb., and Penicillium sp.), and antiprotozoal (Trichomonas vaginalis, Giardia lamblia, and Entamoeba histolytica) effects. To study the anti-rotavirus properties, firstly the 3-(4,5-dimethylthiazol-2-yl)-2-5-diphenyltetrazolium bromide (MTT) method was used to establish the median cytotoxicity concentration (CC 50 ) of the compounds, using MA-104 cell line. Under the experimental conditions used, cytotoxic, anti-rotavirus, antibacterial, and antifungal properties were not observed for these compounds.


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