Peer-reviewed veterinary case report
Semisynthesis of Platensimycin Derivatives with Antibiotic Activities in Mice via Suzuki-Miyaura Cross-Coupling Reactions.
- Journal:
- Journal of medicinal chemistry
- Year:
- 2018
- Authors:
- Deng, Youchao et al.
- Affiliation:
- Xiangya International Academy of Translational Medicine at Central South University · China
- Species:
- rodent
Abstract
Platensimycin (PTM), originally isolated from soil bacteria Streptomyces platensis, is a potent FabF inhibitor against many Gram-positive pathogens, such as methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci. However, the further clinical development of PTM is hampered by its poor pharmacokinetic properties. In this study, 20 PTM derivatives were prepared by Suzuki-Miyaura cross-coupling reactions catalyzed by Pd (0)/C. Compared to PTM, 6-pyrenyl PTM (6t) showed improved antibacterial activity against MRSA in a mouse peritonitis model. Our results support the strategy to target the essential fatty acid synthases in major pathogens, in order to discover and develop new generations of antibiotics.
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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/30461269/