2. Academic Validation
  3. Synthesis and evaluation of antibacterial and antitumor activities of new galactopyranosylated amino alcohols

Synthesis and evaluation of antibacterial and antitumor activities of new galactopyranosylated amino alcohols

  • Eur J Med Chem. 2016 Jan 27:108:203-210. doi: 10.1016/j.ejmech.2015.11.037.
Fábio de Souza Fernandes 1,  Tayrine Silva Fernandes 1,  Lígia Souza da Silveira 1,  Wiliam Caneschi 1,  Maria Cristina S Lourenço 2,  Claudio G Diniz 3,  Pollyanna Francielli de Oliveira 4,  Sabrina de Paula Lima Martins 4,  Daiane Eleutério Pereira 4,  Denise Crispim Tavares 4,  Mireille Le Hyaric 1,  Mauro V de Almeida 1,  Mara Rubia C Couri 5
Affiliations

Affiliations

  • 1 Departamento de Química, ICE, Universidade Federal de Juiz de Fora, Cidade Universitária, 36036-900, Juiz de Fora, MG, Brazil.
  • 2 Instituto de Pesquisa Clínica Evandro Chagas, IPEC, Fundação Oswaldo Cruz, 21041-250, Rio de Janeiro, RJ, Brazil.
  • 3 Departamento de Parasitologia, Microbiologia e Imunologia, ICB, Universidade Federal de Juiz de Fora, 36036-900, Juiz de Fora, MG, Brazil.
  • 4 Laboratório de Mutagênese, Universidade de Franca, Franca, SP, Brazil.
  • 5 Departamento de Química, ICE, Universidade Federal de Juiz de Fora, Cidade Universitária, 36036-900, Juiz de Fora, MG, Brazil. Electronic address: mara.rubia@ufjf.edu.br.
PMID: 26649907 DOI: 10.1016/j.ejmech.2015.11.037
Abstract

Three series of d-galactose derivatives linked to a lipophilic aminoalcohol moiety were synthesized and their Antibacterial activity was evaluated against Mycobacterium tuberculosis and representative species of Gram positive and Gram negative bacteria. Five out of the thirteen tested compounds displayed activity against M. tuberculosis, with a minimal inhibitory concentration (MIC) of 12.5 μg/mL and seven compounds were active against the four Bacterial strains tested. The best results were obtained for amino alcohols 10 and 11 against Staphylococcus epidermidis (MIC = 2 μg/mL). The antitumor activity was evaluated against three tumor cell lines (MCF-7, HeLa and MO59J) and compared to the normal cell line GM07492A. The results showed that the lowest IC50 values were observed for the amino alcohol 16 against MCF-7 (11.9 μM) and MO59J (10.0 μM).

Keywords

antibacterial; antitumor; galactopyranosylated amino alcohols; lipophilicity.

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