2017
DOI: 10.1007/7355_2017_15
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The Oxazolidinones

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Cited by 14 publications
(6 citation statements)
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“…Sutezolid differs from linezolid by having a thiomorpholine substituent and has displayed a better anti-TB activity and improved safety profile compared to linezolid. , In addition, delpazolid ( 3 ) , and TBI-223 ( 4 ) are also under clinical development for the treatment of TB. The development of AZD5847 ( 5 ) by AstraZeneca for the treatment of Gram-positive infections and TB has been discontinued. The long duration required for the treatment of TB with linezolid has been associated with severe side effects such as anemia, thrombocytopenia, and optic and peripheral neuropathy. The toxicity of the oxazolidinone class is thought to be mediated by the inhibition of mitochondrial protein synthesis (MPS) and monoamine oxidase (MAO). Therefore, discovery of new oxazolidinones with an improved safety and efficacy profile is extremely important for the treatment of TB …”
Section: Introductionmentioning
confidence: 99%
“…Sutezolid differs from linezolid by having a thiomorpholine substituent and has displayed a better anti-TB activity and improved safety profile compared to linezolid. , In addition, delpazolid ( 3 ) , and TBI-223 ( 4 ) are also under clinical development for the treatment of TB. The development of AZD5847 ( 5 ) by AstraZeneca for the treatment of Gram-positive infections and TB has been discontinued. The long duration required for the treatment of TB with linezolid has been associated with severe side effects such as anemia, thrombocytopenia, and optic and peripheral neuropathy. The toxicity of the oxazolidinone class is thought to be mediated by the inhibition of mitochondrial protein synthesis (MPS) and monoamine oxidase (MAO). Therefore, discovery of new oxazolidinones with an improved safety and efficacy profile is extremely important for the treatment of TB …”
Section: Introductionmentioning
confidence: 99%
“…In their research, the authors synthesized the siderophore‐cephalosporin‐oxazolidinone conjugate ( 22 , Figure ) by attaching an oxazolidinone ( 23 ) to the 3′‐methyl position of a siderophore‐conjugated cephalosporin. Of note, oxazolidinones target microbial ribosomes, and cannot permeate Gram‐negative OMs nor undergo rapid efflux . Because of this, oxazolidinones are effective as Gram‐positive antibiotics, but are not effective against a majority of Gram‐negative pathogens.…”
Section: Trojan Horse Approaches To Overcome Antimicrobial Resistancementioning
confidence: 99%
“…As such, much effort has been devoted to improving the activity and ADME/T properties of linezolid. Extensive structural modifications along with the structure–activity relationship (SAR) studies were focused on the C-ring and C5 side chain (Figure ) of the parent scaffold. Tedizolid phosphate ( 2 ) was the second oxazolidinone drug approved by FDA for the treatment of MRSA skin infections in 2014 . Contezolid ( 3 ), developed by MicuRx Pharmaceuticals, phase III clinical trials were recently finished and the New Drug Application was submitted to regulators .…”
Section: Introductionmentioning
confidence: 99%