Synthesis, anti-MRSA, and anti-VRE activity of hemin conjugates with amino acids and branched peptides.
CHEMICAL BIOLOGY & DRUG DESIGN(2013)
Abstract
The increasing prevalence of antibiotic-resistant bacterial strains has necessitated the synthesis of novel antibacterial agents. It was previously shown that naturally occurring metalloporphyrin hemin possesses dark antibacterial activity against Gram-positive bacteria. To improve hemin antibacterial activity, we synthesized a number of hemin conjugates with amino acids and branched peptides. Arginine-containing hemin conjugates demonstrated high antibacterial activity against Gram-positive bacteria including methicillin- and vancomycin-resistant strains in vitro. Most of the synthesized conjugates showed low toxicity against human erythrocytes and leukocytes.
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Key words
antibacterial activity,branched peptides,hemin,methicillin-resistant Staphylococcus aureus,vancomycin-resistant Enterococcus faecium
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