Lipidated Peptidomimetics with Improved Antimicrobial Activity

被引:54
作者
Hu, Yaogang [1 ]
Amin, Mohamad Nassir [1 ]
Padhee, Shruti [1 ]
Wang, Rongsheng E. [1 ]
Qiao, Qiao [1 ]
Bai, Ge [1 ]
Li, Yaqong [1 ]
Mathew, Archana [1 ]
Cao, Chuanhai [2 ]
Cai, Jianfeng [1 ]
机构
[1] Univ S Florida, Dept Chem, Tampa, FL 33620 USA
[2] Univ S Florida, Coll Pharm, Tampa, FL 33620 USA
关键词
antimicrobial peptides; peptidomimetics; drug resistance; lipidation; alpha-AApeptides; HOST-DEFENSE PEPTIDES; IN-VITRO; ANTIBACTERIAL ACTIVITIES; GAMMA-AAPEPTIDES; PLAUSIBLE MODE; PEPTOID MIMICS; BETA-PEPTIDES; POLYMYXIN-B; LIPOPEPTIDES; OLIGOMERS;
D O I
10.1021/ml3001215
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
We report a series of lipidated alpha-AApeptides that mimic the structure and function of natural antimicrobial lipopeptides. Several short lipidated alpha-AApeptides show broad-spectrum activity against a range of clinically related Gram-positive and Gram-negative bacteria as well as fungus. Their antimicrobial activity and selectivity are comparable or even superior to the clinical candidate pexiganan as well as previously reported linear alpha-AApeptides. The further development of lipidated alpha-AApeptides will lead to a new class of antibiotics to combat drug resistance.
引用
收藏
页码:683 / 686
页数:4
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