linezolid has been researched along with platensimycin* in 3 studies
3 other study(ies) available for linezolid and platensimycin
| Article | Year |
|---|---|
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
Bacterial fatty acid synthases are promising antibacterial targets against multidrug-resistant pathogens. Platensimycin (PTM) is a potent FabB/FabF inhibitor, while its poor pharmacokinetics hampers the clinical development. In this study, a focused library of PTM derivatives was prepared through thiolysis of PTM oxirane ( Topics: Adamantane; Aminobenzoates; Anilides; Animals; Anti-Bacterial Agents; Humans; Male; Methicillin-Resistant Staphylococcus aureus; Mice; Mice, Inbred C57BL; Models, Molecular; Peritonitis; Small Molecule Libraries; Staphylococcal Infections; Staphylococcus | 2019 |
Biomimetic Stereoselective Sulfa-Michael Addition Leads to Platensimycin and Platencin Sulfur Analogues against Methicillin-Resistant Staphylococcus aureus.
Several sulfur-containing platensimycin (PTM) and platencin (PTN) analogues, with activities comparable to the parent natural products, have recently been discovered from microorganisms, implying a biomimetic route to diversify the PTM and PTN scaffolds for structure-activity relationship study. We present here a substrate-directed and scaleable semisynthetic strategy to make PTM and PTN sulfur analogues with excellent diasteroselectivity, without using any chiral catalysts. Most of the sulfur analogues showed strong activities against clinical Staphylococcus aureus isolates, with minimum inhibitory concentrations of 0.5-2 μg mL Topics: Adamantane; Aminobenzoates; Aminophenols; Anilides; Anti-Bacterial Agents; Biological Products; Biomimetics; Methicillin-Resistant Staphylococcus aureus; Microbial Sensitivity Tests; Polycyclic Compounds; Structure-Activity Relationship; Sulfur | 2018 |
Semisynthesis of Platensimycin Derivatives with Antibiotic Activities in Mice via Suzuki-Miyaura Cross-Coupling Reactions.
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. Topics: Adamantane; Aminobenzoates; Anilides; Animals; Anti-Bacterial Agents; Disease Models, Animal; Male; Methicillin-Resistant Staphylococcus aureus; Microbial Sensitivity Tests; Molecular Docking Simulation; Peritonitis; Staphylococcal Infections | 2018 |