Structure-activity relationship of daptomycin analogues with substitution at (2S, 3R) 3-methyl glutamic acid position
2016; Elsevier BV; Volume: 27; Issue: 3 Linguagem: Inglês
10.1016/j.bmcl.2016.12.046
ISSN1464-3405
AutoresDu’an Lin, Hiu Yung Lam, Wenbo Han, Nicole Cotroneo, Bhaumik A. Pandya, Xuechen Li,
Tópico(s)RNA and protein synthesis mechanisms
ResumoDaptomycin 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.
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