期刊
INTERNATIONAL JOURNAL OF PEPTIDE RESEARCH AND THERAPEUTICS
卷 21, 期 3, 页码 243-247出版社
SPRINGER
DOI: 10.1007/s10989-015-9460-1
关键词
Peptidomimetics; 1, 4-dihydropyridine scaffold; Broad spectrum anti-bacterial; Anti-microbial; Cationic peptides; Drug design
资金
- Authority for Research & Development of Ariel University
We synthesized new broad spectrum antibacterial cationic peptidomimetics centered on a hydrophobic 1,4-dihydropyridine (1,4-DHP) scaffold. The synthesis involves the preparation of the scaffold in a three step Hantzsch reaction followed by simultaneous coupling of the 1,4-DHP scaffold to two dipeptides bearing cationic side chains. The synthesized peptidomimetics were found to have no measurable toxic hemolytic effect against mammalian red blood cells. The compounds were found to have antibacterial activity against Gram-(-) and Gram-(+) bacteria with MICs in the range of 35-100 mu g/mL. These cationic antimicrobial peptidomimetics will lead to more effective antibacterial drug candidates based on a synthetically accessible scaffold.
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