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Lipidated peptidomimetics with improved antimicrobial activity.


ABSTRACT: We report a series of lipidated ?-AApeptides that mimic the structure and function of natural antimicrobial lipopeptides. Several short lipidated ?-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 ?-AApeptides. The further development of lipidated ?-AApeptides will lead to a new class of antibiotics to combat drug resistance.

SUBMITTER: Hu Y 

PROVIDER: S-EPMC4025737 | biostudies-literature | 2012 Aug

REPOSITORIES: biostudies-literature

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Lipidated peptidomimetics with improved antimicrobial activity.

Hu Yaogang Y   Amin Mohamad Nassir MN   Padhee Shruti S   Wang Rongsheng E RE   Qiao Qiao Q   Bai Ge G   Li Yaqong Y   Mathew Archana A   Cao Chuanhai C   Cai Jianfeng J  

ACS medicinal chemistry letters 20120712 8


We report a series of lipidated α-AApeptides that mimic the structure and function of natural antimicrobial lipopeptides. Several short lipidated α-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 α-AApeptides. The further development of lipidated α-AApeptides  ...[more]

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