期刊
MEDCHEMCOMM
卷 4, 期 5, 页码 874-880出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c3md20311e
关键词
-
资金
- CSIR, New Delhi, India
- Council of Scientific and Industrial Research (CSIR) network project [NWP-013]
We report herein, synthesis and mode of action of novel, cell selective, N-terminal tagged tetra-peptide conjugates. Analogues AP1 and AP2 with linoleic acid and p-terphenyl carboxylic acid tagging showed potent activity against Gram-positive and Gram-negative bacterial strains including the clinically relevant pathogen MRSA. For active analogues interaction studies with model bacterial mimic membranes revealed a direct correlation between activity and membrane perturbation. Further, active conjugates showed membrane depolarization and severe bacterial membrane disrupting ability. The hydrophobic-charge-hydrophobic template designed here can be useful in further optimizing end tagged peptidomimetics for therapeutic potential.
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