1202778-95-7Relevant articles and documents
THERAPEUTIC PEPTIDES
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Paragraph 0101, (2013/03/26)
The present invention provides a peptide, peptidomimetic or amino acid derivative having a net positive charge of at least +2 and incorporating a disubstituted β amino acid, each of the substituting groups in the β amino acid, which may be the same or dif
Antimicrobial activity of small β-peptidomimetics based on the pharmacophore model of short cationic antimicrobial peptides
Hansen, Terkel,Alst, Tore,Havelkova, Martina,Str?m, Morten B.
experimental part, p. 595 - 606 (2010/06/19)
We have synthesized a series of small β-peptidomimetics (Mw 2,2-amino acid coupled to a C-terminal L-arginine amide residue. By varying the lipophilic side-chains of the β2,2-amino acids, we obtained a series of highly potent β-peptidomimetics with high enzymatic stability against α-chymotrypsin and a general low toxicity against human erythrocytes. The most potent β-peptidomimetics displayed minimal inhibitory concentrations of 2.1-7.2 μM against Staphylococcus aureus, methicillin resistant Staphylococcus aureus (MRSA), methicillin resistant Staphylococcus epidermidis (MRSE), and Escherichia coli. Small amphipathic β-peptidomimetics may be a promising class of antimicrobial agents by means of having a similar range of potency and selectivity as larger cationic antimicrobial peptides in addition to improved enzymatic stability and lower costs of production.