A combined experimental and theoretical study shows how the interaction of VUV radiation with cyclo-(alanine-alanine), one 2,5-diketopiperazines (DKPs), produces reactive oxazolidinone intermediates. The simulations reveal that these intermediates other neutral charged fragments, released in molecular decomposition, leads either to reconstruction cyclic dipeptide or formation longer linear pept...

The activity of Rivaroxoban oxazolidinone series against Mycobacterium terrae was investigated in silico and vitro. In studies have shown a high binding affinity Rivaroxaban to β-ketoacyl[ACP]synthase I that plays key role the biosynthesis mycolic acids, being components mycobacterial cell wall. molecular docking study, two main sites with protein were predicted evaluated: minimum energies foun...

A method was developed for simultaneous qualitative and quantitative analysis of five metabolites of nitrofuran antibiotics, including 3-amino-2-oxazolidinone (AOZ), 5-morpholino-methyl-3-amino-2-oxazolidinone ( AMOZ ), semicarbazide ( SEM ), 1-aminohydantoin (AHD) and 3, 5-dinitrosalicylic acid hydrazide (DNSH) in aquatic products by liquid chromatography-tandem mass spectrometry (LC-MS/MS). T...

Trifluoromethylated organic compounds, especially chiral quaternary alcohols bearing trifluoromethyl group are of important intermediates in drugs, agrochemicals and etc.An efficient epoxidation of β-CF3-β,β-disubstituted unsaturated ketones (6) has been developed with environmental benign hydrogen peroxide as the oxidant and F5-substituted chiral qua...

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...