نتایج جستجو برای: oxazolidinone
تعداد نتایج: 557 فیلتر نتایج به سال:
This thesis documents the design and synthesis of chiral amino alcohol monomers 161, 162,167, chiral oxazolidine monomer 168 and chiral oxazolidinone monomers 203 and 204. The synthetic strategy relies on the key Suzuki coupling of aryl triflates derived from tyrosine with p-vinylphenylboronic acid where the resultant vinyl monomers are further modified to provide the desired functionality. / M...
The emergence of multidrug-resistant pathogens will make current antibiotics ineffective. For linezolid, a member of the novel oxazolidinone class of antibiotics, 10 nucleotide mutations in the ribosome have been described conferring resistance. Hypotheses for how these mutations affect antibiotics binding have been derived based on comparative crystallographic studies. However, a detailed desc...
Derivatives of the two unusual 8-hydroxy amino acids in echinocandin D (1) have been synthesized by employing asymmetric glycine enolate aldol methodology. The N-Boc,O-benzyl derivative of (2S,3R)-3-hydroxyhomotyrosine (Hht) (2) and the methyl ester of (2.9,3S,4.9)-3-hydroxy-4-methylproline (Hmp) (3) have been synthesized in four steps each from (isothiocyanoacety1)oxazolidinone 4 and (bromoace...
Staphylococcal resistance to linezolid (LZD) is mediated through ribosomal mutations (23S rRNA or ribosomal proteins L3 and L4) or through methylation of 23S rRNA by the horizontally transferred Cfr methyltransferase. To investigate the structural basis for oxazolidinone activity against LZD-resistant (LZD(r)) strains, we compared structurally diverse, clinically relevant oxazolidinones, includ...
Linezolid, the first oxazolidinone to be used clinically, is effective in the treatment of infections caused by various Gram-positive pathogens, including multidrug resistant enterococci and methicillin-resistant Staphylococus aureus. It has been used successfully for the treatment of patients with endocarditis and bacteraemia, osteomyelitis, joint infections and tuberculosis and it is often us...
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