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Synthesis,Anti‐MRSA,and Anti‐VRE Activity of Hemin Conjugates with Amino Acids and Branched Peptides
Authors:Sergei A Okorochenkov  Galina A Zheltukhina  Elena P Mirchink  Elena B Isakova  Alexey V Feofanov  Vladimir E Nebolsin
Institution:1. Department of Biotechnology and Organic synthesis, Moscow State University of Fine Chemical Technology, , 119571 Moscow, Russia;2. Gause Institute of New Antibiotics, Russian Academy of Medical Sciences, , 119021 Moscow, Russia;3. M.M. Shemyakin and Yu.A. Ovchinnikov Institute of bioorganic chemistry, , 117997 Moscow, Russia;4. LTD “Pharmenterprises”, , 119571 Moscow, Russia
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.
Keywords:antibacterial activity  branched peptides  hemin  methicillin‐resistant Staphylococcus aureus  vancomycin‐resistant Enterococcus faecium
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