| Literature DB >> 26649907 |
Fábio de Souza Fernandes1, Tayrine Silva Fernandes1, Lígia Souza da Silveira1, Wiliam Caneschi1, Maria Cristina S Lourenço2, Claudio G Diniz3, Pollyanna Francielli de Oliveira4, Sabrina de Paula Lima Martins4, Daiane Eleutério Pereira4, Denise Crispim Tavares4, Mireille Le Hyaric1, Mauro V de Almeida1, Mara Rubia C Couri5.
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).Entities:
Keywords: antibacterial; antitumor; galactopyranosylated amino alcohols; lipophilicity
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Year: 2015 PMID: 26649907 DOI: 10.1016/j.ejmech.2015.11.037
Source DB: PubMed Journal: Eur J Med Chem ISSN: 0223-5234 Impact factor: 6.514