de Souza Fernandes Fábio, Fernandes Tayrine Silva, da Silveira Lígia Souza, Caneschi Wiliam, Lourenço Maria Cristina S, Diniz Claudio G, de Oliveira Pollyanna Francielli, Martins Sabrina de Paula Lima, Pereira Daiane Eleutério, Tavares Denise Crispim, Le Hyaric Mireille, de Almeida Mauro V, Couri Mara Rubia C
Departamento de Química, ICE, Universidade Federal de Juiz de Fora, Cidade Universitária, 36036-900, Juiz de Fora, MG, Brazil.
Instituto de Pesquisa Clínica Evandro Chagas, IPEC, Fundação Oswaldo Cruz, 21041-250, Rio de Janeiro, RJ, Brazil.
Eur J Med Chem. 2016 Jan 27;108:203-210. doi: 10.1016/j.ejmech.2015.11.037. Epub 2015 Nov 24.
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).
合成了与亲脂性氨基醇部分相连的三个系列的D-半乳糖衍生物，并评估了它们对结核分枝杆菌以及革兰氏阳性和革兰氏阴性细菌代表性菌株的抗菌活性。在所测试的13种化合物中，有5种对结核分枝杆菌有活性，最低抑菌浓度（MIC）为12.5μg/mL，7种化合物对所测试的四种细菌菌株有活性。氨基醇10和11对表皮葡萄球菌的效果最佳（MIC = 2μg/mL）。评估了其对三种肿瘤细胞系（MCF-7、HeLa和MO59J）的抗肿瘤活性，并与正常细胞系GM07492A进行了比较。结果表明，氨基醇16对MCF-7（11.9μM）和MO59J（10.0μM）的IC50值最低。
