Literature DB >> 26649907

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

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).
Copyright © 2015 Elsevier Masson SAS. All rights reserved.

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


  1 in total

1.  Unprecedented Convergent Synthesis of Sugar-Functionalization of Phosphinic Acids under Metal-Free Conditions.

Authors:  Moaz M Abdou; Paul M O'Neill; Eric Amigues; Magdalini Matziari
Journal:  ACS Omega       Date:  2022-06-16
  1 in total

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