Treatments for Clostridium difficile infection remain limited, despite the introduction of fidaxomicin, and development of new agents is necessary. We determined the in vitro susceptibilities of 199 prevalent or emerging Clostridium difficile PCR ribotypes to MCB3681, a novel investigational quinolonyl-oxazolidinone, and 8 comparators (metronidazole, vancomycin, fidaxomicin, moxifloxacin, cipro...

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...

Linezolid is an oxazolidinone antibiotic with weak monoamine oxidase (MAO) type A and MAO type B inhibitory effects. Linezolid has been associated with serotonin toxicity when used concomitantly with multiple medications that are known to increase serotonin concentrations. We report the case of a 65-year-old woman with signs and symptoms of serotonin toxicity following administration of linezol...

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)°.

due to high resolution power of sulfated cyclodextrins (hs-cds), utilization of these selectors for chiral resolution of 7 basic and 2 zwitterionic drugs have been examined. experiments were performed on a hp3dce instrument equipped with an on-column diode array uv absorbance detector. fused silica capillaries with an inner diameter of 50 ?m, an outer diameter of 365 ?m, and a total length of 4...

chiral pyrrolidines and pyrrolizidines with spirooxindole ring systems are the central skeletons for numerous alkaloids and pharmacologically important compounds. gelesmine, pseudotabersonine, formosanine, isoformosanine, morroniside and mitraphylline are some of the alkaloids containing spirooxindole ring systems. derivatives of spirooxindole find very wide biological applications as anti micr...

the distribution behavior of ofloxacin enantiomers was examined in the aqueous and organic solvent of a two-phase system containing chiral selector l-tartarate. the effect of extraction equilibrium time, buffer ph, organic solvents and length of alkyl chain of l-tartarate on the partition coefficients and enantioselectivity of racemic ofloxacin were investigated, respectively. the l-tartarate f...