RWJ-416457, a novel oxazolidinone, had modal MICs of 0.5 to 1 microg/ml for linezolid-susceptible staphylococci and enterococci, versus linezolid MICs for these organisms of 1 or 2 microg/ml. RWJ-416457 MICs for mutants with 23S rRNA mutations were 2 to 32 microg/ml, versus linezolid MICs of 8 to 64 microg/ml; actual values reflected the proportion of gene copies mutated.

LCB01-0371 is a new oxazolidinone with cyclic amidrazone. In vitro activity of LCB01-0371 against 624 clinical isolates was evaluated and compared with those of linezolid, vancomycin, and other antibiotics. LCB01-0371 showed good activity against Gram-positive pathogens. In vivo activity of LCB01-0371 against systemic infections in mice was also evaluated. LCB01-0371 was more active than linezo...

The absolute structure of the chiral asymmetric indole precursor title compound, C11H13NO3S, was confirmed by refinement of the Flack and Hooft parameters and is that expected based on the starting materials for the synthesis. The phenyl group subtends a dihedral angle of 56.40 (5)° with the mean plane of the oxazolidinone ring, which adopts an envelope conformation, with the C atom bearing the...

The new oxazolidinone antimicrobial, linezolid, has been approved for the treatment of infections caused by various gram-positive bacteria, including meticillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE). Although instances of linezolid resistance in VRE have been reported, resistance has not been encountered among clinical isolates of S aureus. We have ch...

Free chlorine and a combined organic N-chloramine (3-chloro-4,4-dimethyl-2-oxazolidinone, compound 1) were compared for efficacy as disinfectants against an admixture of cysts of Giardia lamblia and Giardia canis in water solution under a variety of test conditions; variables were pH, temperature, and water quality. In general, compound 1 was found to reduce the giardial excystation in the solu...

In the title compound, C(21)H(23)NO(3), the central oxazolidinone ring is approximately planar, the maximum deviation from the plane through the central ring being 0.043 (1) Å. The tert-butyl and benzyl substituents are cis to each other and trans to the N-benzoyl group. The inter-planar angle between the aromatic rings of the C-benzyl and N-benzoyl groups is 81.10 (4)°.

The stereocontrolled synthesis of trans-disubstituted cyclopropylketones has been achieved from beta-alkyl, gamma-benzoyl phosphine oxides via a three-step cascade reaction incorporating an acyl transfer, phosphinoyl transfer and cyclisation to form the cyclopropane. Using Evans' chiral oxazolidinone auxiliary and by masking the phosphine oxide moiety as a phosphine borane we have extended the ...

The susceptibilities of clinical vancomycin-intermediate Staphylococcus aureus (VISA), heterogeneous VISA, and laboratory-generated linezolid-resistant S. aureus strains to the new oxazolidinone AZD2563 were assessed by agar dilution MIC determination. All clinical strains were susceptible to linezolid, and the linezolid MICs for them were equal to or twofold higher than those of AZD2563. Cross...

Table of Contents General methods S1 Reagents and materials S2 General protocol for the preparation of starting chiral ynamides S3 General procedures for the allylation of stereodefined trisubstituted copper enolate S5 Optimization reactions S8 Products of the enantioselective allylic alkylation reaction S9 Cleavage of oxazolidinone moiety 4 S19 References S21 X-Ray crystallographic analysis da...

The formal synthesis of (+)-3-epi-eupomatilone-6 () and the 3,5-bis-epimer () has been accomplished. The key synthetic strategy involved the stereoselective construction of (3R,4S,5R)- and (3R,4S,5S)-trisubstituted γ-butyrolactones and from (2R,3R)-2,3-dimethyl-4-pentenoic acid derivative , which was readily obtained via stereoselective conjugate addition of vinylmagnesium chloride to a chiral ...