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Resistance to methicillin is conferred by activation of a new bacterial penicillin binding protein (PBP) mecA gene. This encodes protein PBP2a. PBP2a works in a similar manner to other PBPs, but it binds β-lactams with very low affinity, meaning they do not compete efficiently with the natural substrate...
A c14-modified pleuromutilin derivative, its preparation method and use in the treatment of bacterial infections
PendingCN122102979AAntibacterial agentsSulfonic acid esters preparationMulti resistant bacteriaAntimicrobial drug
The present application belongs to the field of pharmaceutical chemistry and antibacterial drug technology, and particularly relates to a C14 modified pleuromutilin derivative, a preparation method thereof and application thereof in treating gram-positive bacteria, especially gram-positive drug-resistant bacterial infection. The C14 modified pleuromutilin derivative provided by the present application has a structure shown in formula I or formula II. The present application introduces a heterocyclic side chain (4-trifluoromethylphenylthiol or 1-(4,5-dihydrothiazole-2-yl)azetidine-3-thiol) at the C14 site of pleuromutilin to synthesize the C14 modified pleuromutilin derivative, which significantly enhances the antibacterial activity of the C14 modified pleuromutilin derivative on methicillin-resistant Staphylococcus aureus (MRSA) and cfr gram-positive bacterial strains, and has high drug resistance barrier, low cytotoxicity and hemolyticity. The C14 modified pleuromutilin derivative provided by the present application is suitable for treating multiple drug-resistant bacterial infection in veterinary and human medicine. Formula I, formula II.
Owner:POULTRY INSTITUTE SHANDONG ACADEMY OF AGRICULTURAL SCIENCE (SHANDONG SPECIFIC PATHOGEN FREE CHICKS RESEARCH CENTER)