达托霉素类似物在（2S，3R）3-甲基谷氨酸位置进行取代的构效关系。
Structure-activity relationship of daptomycin analogues with substitution at (2S, 3R) 3-methyl glutamic acid position.
作者信息
Lin Du'an, Lam Hiu Yung, Han Wenbo, Cotroneo Nicole, Pandya Bhaumik A, Li Xuechen
机构信息
Department of Chemistry, State Key Laboratory of Synthetic Chemistry, The University of Hong Kong, Hong Kong Special Administrative Region.
Cubist Pharmaceutical, Inc., 65 Hayden Avenue, Lexington, MA 02421, United States.
出版信息
Bioorg Med Chem Lett. 2017 Feb 1;27(3):456-459. doi: 10.1016/j.bmcl.2016.12.046. Epub 2016 Dec 18.
Daptomycin is a highly effective lipopeptide antibiotic against Gram-positive pathogens. The presence of (2S, 3R) 3-methyl glutamic acid (mGlu) in daptomycin has been found to be important to the antibacterial activity. However the role of (2S, 3R) mGlu is yet to be revealed. Herein, we reported the syntheses of three daptomycin analogues with (2S, 3R) mGlu substituted by (2S, 3R) methyl glutamine (mGln), dimethyl glutamic acid and (2S, 3R) ethyl glutamic acid (eGlu), respectively, and their antibacterial activities. The detailed synthesis of dimethyl glutamic acid was also reported.
达托霉素是一种针对革兰氏阳性病原体的高效脂肽类抗生素。已发现达托霉素中（2S，3R）3-甲基谷氨酸（mGlu）的存在对抗菌活性很重要。然而，（2S，3R）mGlu的作用尚未明确。在此，我们报道了三种达托霉素类似物的合成及其抗菌活性，这三种类似物中（2S，3R）mGlu分别被（2S，3R）甲基谷氨酰胺（mGln）、二甲基谷氨酸和（2S，3R）乙基谷氨酸（eGlu）取代。还报道了二甲基谷氨酸的详细合成方法。
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