linezolid and platencin

linezolid has been researched along with platencin* in 2 studies

Other Studies

2 other study(ies) available for linezolid and platencin

Article	Year
Biomimetic Stereoselective Sulfa-Michael Addition Leads to Platensimycin and Platencin Sulfur Analogues against Methicillin-Resistant Staphylococcus aureus. Journal of natural products, 2018, 02-23, Volume: 81, Issue:2 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
Discovery of platencin, a dual FabF and FabH inhibitor with in vivo antibiotic properties. Proceedings of the National Academy of Sciences of the United States of America, 2007, May-01, Volume: 104, Issue:18 Emergence of bacterial resistance is a major issue for all classes of antibiotics; therefore, the identification of new classes is critically needed. Recently we reported the discovery of platensimycin by screening natural product extracts using a target-based whole-cell strategy with antisense silencing technology in concert with cell free biochemical validations. Continued screening efforts led to the discovery of platencin, a novel natural product that is chemically and biologically related but different from platensimycin. Platencin exhibits a broad-spectrum Gram-positive antibacterial activity through inhibition of fatty acid biosynthesis. It does not exhibit cross-resistance to key antibiotic resistant strains tested, including methicillin-resistant Staphylococcus aureus, vancomycin-intermediate S. aureus, and vancomycin-resistant Enterococci. Platencin shows potent in vivo efficacy without any observed toxicity. It targets two essential proteins, beta-ketoacyl-[acyl carrier protein (ACP)] synthase II (FabF) and III (FabH) with IC50 values of 1.95 and 3.91 microg/ml, respectively, whereas platensimycin targets only FabF (IC50 = 0.13 microg/ml) in S. aureus, emphasizing the fact that more antibiotics with novel structures and new modes of action can be discovered by using this antisense differential sensitivity whole-cell screening paradigm. Topics: 3-Oxoacyl-(Acyl-Carrier-Protein) Synthase; Aminophenols; Anti-Bacterial Agents; Enzyme Inhibitors; Microbial Viability; Molecular Structure; Polycyclic Compounds	2007

Article

Year

Biomimetic Stereoselective Sulfa-Michael Addition Leads to Platensimycin and Platencin Sulfur Analogues against Methicillin-Resistant Staphylococcus aureus.

Journal of natural products, 2018, 02-23, Volume: 81, Issue:2

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

Discovery of platencin, a dual FabF and FabH inhibitor with in vivo antibiotic properties.

Proceedings of the National Academy of Sciences of the United States of America, 2007, May-01, Volume: 104, Issue:18

Emergence of bacterial resistance is a major issue for all classes of antibiotics; therefore, the identification of new classes is critically needed. Recently we reported the discovery of platensimycin by screening natural product extracts using a target-based whole-cell strategy with antisense silencing technology in concert with cell free biochemical validations. Continued screening efforts led to the discovery of platencin, a novel natural product that is chemically and biologically related but different from platensimycin. Platencin exhibits a broad-spectrum Gram-positive antibacterial activity through inhibition of fatty acid biosynthesis. It does not exhibit cross-resistance to key antibiotic resistant strains tested, including methicillin-resistant Staphylococcus aureus, vancomycin-intermediate S. aureus, and vancomycin-resistant Enterococci. Platencin shows potent in vivo efficacy without any observed toxicity. It targets two essential proteins, beta-ketoacyl-[acyl carrier protein (ACP)] synthase II (FabF) and III (FabH) with IC50 values of 1.95 and 3.91 microg/ml, respectively, whereas platensimycin targets only FabF (IC50 = 0.13 microg/ml) in S. aureus, emphasizing the fact that more antibiotics with novel structures and new modes of action can be discovered by using this antisense differential sensitivity whole-cell screening paradigm.

Topics: 3-Oxoacyl-(Acyl-Carrier-Protein) Synthase; Aminophenols; Anti-Bacterial Agents; Enzyme Inhibitors; Microbial Viability; Molecular Structure; Polycyclic Compounds

2007