Article ID Journal Published Year Pages File Type
1393847 European Journal of Medicinal Chemistry 2016 8 Pages PDF
Abstract

•A series of fifteen new galactopyranosylated amino alcohols were synthesized.•The compounds were evaluated against Mycobacterium tuberculosis and Gram positive and negative bacteria.•Two amino alcohols were active against S. epidermidis (MIC = 2 μg/mL).•Antitumor activity was evaluated against three tumor cell lines.•Compound 16 showed the lowest IC50 against MCF-7 (11.9 μM) and MO59J (10.0 μM).

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).

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