Dushin Russell G, Wang Ting-Zhong, Sum Phaik-Eng, He Haiyin, Sutherland Alan G, Ashcroft Joseph S, Graziani Edmund I, Koehn Frank E, Bradford Patricia A, Petersen Peter J, Wheless Karen L, How David, Torres Nancy, Lenoy Eileen B, Weiss William J, Lang Stanley A, Projan Steven J, Shlaes David M, Mansour Tarek S
Wyeth Research, Chemical and Screening Sciences, Medicinal Chemistry, Pearl River, NY 10965, USA.
J Med Chem. 2004 Jul 1;47(14):3487-90. doi: 10.1021/jm049765y.
The effect of introducing hydrophobic groups onto the disaccharide portion of the mannopeptimycins has been examined. Under acid-catalyzed conditions dimethyl acetals and ketals react on the terminal mannose of the disaccharide moiety of mannopeptimycin-alpha and the cyclohexylalanyl analogue 2. The preferentially formed monofunctionalized 4,6-acetals and -ketals display potent antibacterial activities against Gram-positive microorganisms, including MRSA, PRSP, and VRE pathogens.
已对在甘露肽霉素的二糖部分引入疏水基团的效果进行了研究。在酸催化条件下，二甲基缩醛和缩酮与甘露肽霉素-α及环己基丙氨酰类似物2的二糖部分的末端甘露糖发生反应。优先形成的单官能化4,6-缩醛和缩酮对革兰氏阳性微生物，包括耐甲氧西林金黄色葡萄球菌（MRSA）、青霉素耐药肺炎链球菌（PRSP）和耐万古霉素肠球菌（VRE）病原体，显示出强效抗菌活性。
