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The Activity of Small Urea‐γ‐AApeptides Toward Gram‐Positive Bacteria
Author(s) -
Su Ma,
Shi Yan,
Wang Minghui,
Gao Ruixuan,
Wu Jianfeng,
Xu Hai,
Xi Chuanwu,
Cai Jianfeng
Publication year - 2019
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201900520
Subject(s) - bacteria , antimicrobial , urea , antibiotics , chemistry , gram negative bacteria , gram positive bacteria , microbiology and biotechnology , combinatorial chemistry , biochemistry , biology , gene , escherichia coli , genetics
Abstract Host Defense Peptides (HDPs) have gained considerable interest due to the omnipresent threat of bacterial infection as a serious public health concern. However, development of HDPs is impeded by several drawbacks, such as poor selectivity, susceptibility to proteolytic degradation, low‐to‐moderate activity and requiring complex syntheses. Herein we report a class of lipo‐linear α/urea‐γ‐AApeptides with a hybrid backbone and low molecular weight. The heterogeneous backbone not only enhances chemodiversity, but also shows effective antimicrobial activity against Gram‐positive bacteria and is capable of disrupting bacterial membranes and killing bacteria rapidly. Given their low molecular weight and ease of access via facile synthesis, they could be practical antibiotic agents.