奎宁酸衍生物的烷基化二胺和两亲性酰胺的合成及其抗菌活性
Synthesis and Antibacterial Activity of Alkylated Diamines and Amphiphilic Amides of Quinic Acid Derivatives.
作者信息
Rezende Celso O, Oliveira Larissa A, Oliveira Bruno A, Almeida Camila G, Ferreira Bianca S, Le Hyaric Mireille, Carvalho Guilherme S L, Lourenço Maria Cristina S, Batista Michel, Marchini Fabricio K, Silva Vânia L, Diniz Claudio G, Almeida Mauro V
机构信息
Departamento de Química, Universidade Federal de Juiz de Fora, 36036-330, Juiz de Fora, MG, Brazil.
Instituto Nacional de Infectologia Evandro Chagas-Fiocruz, 21040-360, Rio de Janeiro, RJ, Brazil.
出版信息
Chem Biol Drug Des. 2015 Sep;86(3):344-50. doi: 10.1111/cbdd.12498. Epub 2015 Jan 20.
Different series of N-alkylated diamines and their derivatives condensed to quinic acid were synthesized and tested for antibacterial properties against Staphylococcus aureus, Staphylococcus epidermidis, Pseudomonas aeruginosa, and Mycobacterium tuberculosis. The lipophilic chain and carbohydrate moiety modulate the antibacterial activity and the compounds showed a structure-activity relationship. Overall, 11 compounds displayed better activity than chloramphenicol against Gram-positive and Gram-negative bacteria. Monoalkylated amines 2a-h displayed an activity similar to that of ethambutol against Mycobacterium tuberculosis.
合成了不同系列的与奎尼酸缩合的N-烷基化二胺及其衍生物，并测试了它们对金黄色葡萄球菌、表皮葡萄球菌、铜绿假单胞菌和结核分枝杆菌的抗菌性能。亲脂性链和碳水化合物部分调节抗菌活性，这些化合物呈现出构效关系。总体而言，11种化合物对革兰氏阳性菌和革兰氏阴性菌的活性优于氯霉素。单烷基化胺2a-h对结核分枝杆菌的活性与乙胺丁醇相似。
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