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Synthesis and evaluation of arylamidine derivatives for new antimicrobial and cytotoxic activities.
Monte, Zenaide S; Silva, Amanda M; Lima, Gláucia M S; Silva, Teresinha G DA; Marques, Karla M R; Rodrigues, Maria D; Falcão, Emerson P S; Melo, Sebastião J.
Affiliation
  • Monte ZS; Programa de Pós-Graduação em Ciências Farmacêuticas, Departamento de Ciências Farmacêuticas, Universidade Federal de Pernambuco/UFPE, Av. Prof. Moraes Rego, 1235, Cidade Universitária, 50740-560 Recife, PE, Brazil.
  • Silva AM; Departamento de Biomedicina, Universidade Federal de Pernambuco/UFPE, Av. Prof. Moraes Rego, 1235, Cidade Universitária, 50740-560 Recife, PE, Brazil.
  • Lima GMS; Departamento de Antibióticos, Universidade Federal de Pernambuco/UFPE, Av. Prof. Moraes Rego, 1235, Cidade Universitária, 50740-560 Recife, PE, Brazil.
  • Silva TGD; Departamento de Antibióticos, Universidade Federal de Pernambuco/UFPE, Av. Prof. Moraes Rego, 1235, Cidade Universitária, 50740-560 Recife, PE, Brazil.
  • Marques KMR; Departamento de Antibióticos, Universidade Federal de Pernambuco/UFPE, Av. Prof. Moraes Rego, 1235, Cidade Universitária, 50740-560 Recife, PE, Brazil.
  • Rodrigues MD; Departamento de Antibióticos, Universidade Federal de Pernambuco/UFPE, Av. Prof. Moraes Rego, 1235, Cidade Universitária, 50740-560 Recife, PE, Brazil.
  • Falcão EPS; Departamento de Nutrição, Núcleo de Nutrição da Universidade Federal de Pernambuco (CAV - UFPE), Rua Alto do Reservatório, Bela Vista, s/n, 55608-680 Cidade Vitoria de Santo Antão, PE, Brazil.
  • Melo SJ; Programa de Pós-Graduação em Ciências Farmacêuticas, Departamento de Ciências Farmacêuticas, Universidade Federal de Pernambuco/UFPE, Av. Prof. Moraes Rego, 1235, Cidade Universitária, 50740-560 Recife, PE, Brazil.
An Acad Bras Cienc ; 89(2): 1051-1059, 2017.
Article in En | MEDLINE | ID: mdl-28640352
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.
Subject(s)

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Candida albicans / Amidines / Gram-Negative Bacteria / Anti-Infective Agents Limits: Humans Language: En Journal: An Acad Bras Cienc Year: 2017 Document type: Article Affiliation country: Brazil Country of publication: Brazil

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Candida albicans / Amidines / Gram-Negative Bacteria / Anti-Infective Agents Limits: Humans Language: En Journal: An Acad Bras Cienc Year: 2017 Document type: Article Affiliation country: Brazil Country of publication: Brazil