Category: oxazolidine

Cho, Yong-Soon published the artcileSingle-dose Intravenous Safety, Tolerability, and Pharmacokinetics and Absolute Bioavailability of LCB01-0371, Related Products of oxazolidine, the publication is Clinical Therapeutics (2019), 41(1), 92-106, database is CAplus and MEDLINE.

LCB01-0371 is a novel broad-spectrum oxazolidinone antibacterial agent under investigation for the treatment of infection by gram-pos. pathogens, including methicillin-resistant Staphylococcus aureus. This study evaluated the safety, tolerability, and pharmacokinetics of LCB01-0371 after a single i.v. (IV) infusion and determined its absolute oral bioavailability at a therapeutic dose of 800 mg.: This study was conducted in 2 parts. The first part was a single-blind, placebo-controlled, escalating single IV dose study (200, 400, 800, and 1200 mg) of LCB01-0371 via 2 different infusion regimens (250 mL over 60 min or 150 mL over 30 min) in 36 healthy male volunteers. The second part was an open-label, 2-way crossover design study in which 8 subjects were randomly assigned to 1 of 2 sequences of a single oral (800 mg) or IV (400 mg) administration of LCB01-0371. Safety assessments were conducted at regular intervals. Blood and urine were serially sampled, and drug concentrations were measured for up to 24 h to calculate pharmacokinetic parameters. LCB01-0371 after IV administration was generally safe and well tolerated up to 800 mg regardless of the infusion regimen. Adverse events were mild, excluding nausea at the highest dose, and resolved spontaneously. After a single IV administration, LCB01-0371 exhibited linear pharmacokinetic properties over the range of 200-800 mg. The elimination t_1/2, volume of distribution, and clearance ranged from 1.48 to 1.68 h, 57.74-76.72 L, and 33.17-43.31 L/h, resp., and they remained unchanged over the corresponding dose range. C_max, AUC_0-last, and AUC_{0-�/sub> increased in a dose-dependent manner. The dose-normalized total exposure after single PO and IV dosing were equivalent, with 90% CIs of the geometric least squares mean ratio of 86.6%-110% for AUC0-last and 86.6%-111% for AUC0-�/sub>. The dose-normalized Cmax was not equivalent between oral and IV dosing, with a 90% CI of the geometric least squares mean ratio of 50.0%-105%. The absolute oral bioavailability of LCB01-0371 after a single 800-mg dose was 99.75%. After a single IV administration, LCB01-0371 was well tolerated in healthy volunteers at doses up to 800 mg, and it exhibited linear pharmacokinetic properties. The comparable total systemic exposure between IV and oral administration supports the ability to switch administration routes without a need for dose adjustment. ClinicalTrials.gov identifier: NCT02882789.}

Clinical Therapeutics published new progress about 1219707-39-7. 1219707-39-7 belongs to oxazolidine, auxiliary class Other Aliphatic Heterocyclic,Oxazolidine,Chiral,Fluoride,Benzene,Amide,Alcohol,Anti-infection, name is (R)-3-(3-Fluoro-4-(1-methyl-5,6-dihydro-1,2,4-triazin-4(1H)-yl)phenyl)-5-(hydroxymethyl)oxazolidin-2-one, and the molecular formula is C14H17FN4O3, Related Products of oxazolidine.

Referemce:
https://en.wikipedia.org/wiki/Oxazolidine,
Oxazolidine | C3H7NO – PubChem

Cho, Yong-Soon published the artcileMultiple-dose Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Oral LCB01-0371 in Healthy Male Volunteers, SDS of cas: 1219707-39-7, the publication is Clinical Therapeutics (2018), 40(12), 2050-2064, database is CAplus and MEDLINE.

LCB01-0371 is a novel oxazolidinone broad-spectrum antibacterial that is more potent than linezolid against systemic infections in animals. The goal of this investigation was to evaluate the pharmacokinetics, pharmacodynamics, safety, and tolerability of multiple-dose LCB01-0371 as well as the pharmacokinetic characteristics of a new 400-mg tablet formulation.: Thirty-two healthy male subjects received BID 400-1600 mg multiple oral dosing of LCB01-0371 (200-mg tablet or 400-mg tablet) for 7 days, and 6 subjects received an 800-mg single oral dose of LCB01-0371 (400-mg tablet). Safety assessments were undertaken at regular intervals. Blood and urine were sampled, and drug concentration and inhibitory and bactericidal titers were measured.LCB01-0371 was generally safe and well tolerated up to 1200 mg BID for 7 days. Adverse events were mild, except for headache, nausea, and dizziness at the dose of 1600 mg, and resolved spontaneously. LCB01-0371 was absorbed rapidly within 2 h after administration, and its accumulation observed on day 7 ranged between 1.10- and 1.46-fold. The elimination t1/2 was 1.64-1.94 h, which remained unchanged across all doses. AUC_0-12 and C_max were not dose proportional across the dose range from 400 to 1200 mg after both single and multiple dosing, indicating a nonlinear pharmacokinetic profile. The percentage of the dose excreted via the urine ranged from 7.84% to 8.95%. The new (400-mg tablet) formulation exhibited less interindividual variability with pharmacokinetic characteristics similar to the original formulation (200-mg tablet). LCB01-0371 exhibited both early serum inhibitory and bactericidal activities against the 4 strains tested in the ex vivo pharmacodynamics study.BID doses of LCB01-0371 up to 1200 mg for 7 days were well tolerated and exhibited rapid serum inhibitory and bactericidal activities against common gram-pos. pathogens. The results warrant further clin. investigation of the antibacterial effect of BID LCB01-0371 administration.

Clinical Therapeutics published new progress about 1219707-39-7. 1219707-39-7 belongs to oxazolidine, auxiliary class Other Aliphatic Heterocyclic,Oxazolidine,Chiral,Fluoride,Benzene,Amide,Alcohol,Anti-infection, name is (R)-3-(3-Fluoro-4-(1-methyl-5,6-dihydro-1,2,4-triazin-4(1H)-yl)phenyl)-5-(hydroxymethyl)oxazolidin-2-one, and the molecular formula is C14H17FN4O3, SDS of cas: 1219707-39-7.

Referemce:
https://en.wikipedia.org/wiki/Oxazolidine,
Oxazolidine | C3H7NO – PubChem

Cho, Yong-Soon published the artcilePharmacokinetics, pharmacodynamics, and tolerability of single-dose oral LCB01-0371, a novel oxazolidinone with broad-spectrum activity, in healthy volunteers, Safety of (R)-3-(3-Fluoro-4-(1-methyl-5,6-dihydro-1,2,4-triazin-4(1H)-yl)phenyl)-5-(hydroxymethyl)oxazolidin-2-one, the publication is Antimicrobial Agents and Chemotherapy (2018), 62(7), e00451-18/1-e00451-18/11, database is CAplus and MEDLINE.

The objectives of this study were to evaluate its safety, tolerability, pharmacokinetics, and pharmacodynamics following single ascending doses. Single oral doses of 600 mg linezolid, a placebo, or LCB01-0371 of between 50 mg and 3,200 mg were tested in 69 healthy male subjects. Blood and urine were sampled, LCB01-0371 concentrations were measured, and the serum inhibitory and bactericidal titers of LCB01-0371 and linezolid were determined LCB01-0371 was well tolerated up to 2,400 mg. The most common drugrelated clin. and laboratory adverse events were nausea with or without vomiting, decreased neutrophil counts, and increased total bilirubin levels. The systemic exposure was approx. dose proportional over the range of 50 mg to 800 mg, which includes the anticipated clin. dose. The mean clearance, renal clearance, and volume of distribution were significantly decreased at higher doses (above 800 mg). LCB01-0371 exhibited early bacteriostatic activity against all tested strains except for Streptococcus pneumoniae strains, and the potency of LCB01-0371 at 800 mg was similar to that of linezolid at the therapeutic dose (600 mg). However, LCB01-0371 had less bactericidal activity than linezolid. Taken together, LCB01-0371 was well tolerated, exhibited approx. dose proportionality within the anticipated clin. relevant dose range, and showed bacteriostatic and bactericidal activity comparable to that of linezolid. These results support the further clin. development of LCB01-0371.

Antimicrobial Agents and Chemotherapy published new progress about 1219707-39-7. 1219707-39-7 belongs to oxazolidine, auxiliary class Other Aliphatic Heterocyclic,Oxazolidine,Chiral,Fluoride,Benzene,Amide,Alcohol,Anti-infection, name is (R)-3-(3-Fluoro-4-(1-methyl-5,6-dihydro-1,2,4-triazin-4(1H)-yl)phenyl)-5-(hydroxymethyl)oxazolidin-2-one, and the molecular formula is C14H17FN4O3, Safety of (R)-3-(3-Fluoro-4-(1-methyl-5,6-dihydro-1,2,4-triazin-4(1H)-yl)phenyl)-5-(hydroxymethyl)oxazolidin-2-one.

Referemce:
https://en.wikipedia.org/wiki/Oxazolidine,
Oxazolidine | C3H7NO – PubChem

Anthony, David published the artcileNickel-Catalyzed Asymmetric Reductive Diarylation of Vinylarenes, Application of (4S,4’S)-4,4′-Diisobutyl-4,4′,5,5′-tetrahydro-2,2′-bioxazole, the publication is Angewandte Chemie, International Edition (2019), 58(10), 3198-3202, database is CAplus and MEDLINE.

A nickel-catalyzed asym. diarylation reaction of vinylarenes enabled the preparation of chiral α,α,β-triarylated ethane scaffolds, which existed in a number of biol. active mols. The use of reducing conditions with aryl bromides as coupling partners obviated the need for stoichiometric organometallic reagents and tolerated a broad range of functional groups. The application of an N-oxyl radical as a ligand to a nickel catalyst represented a novel approach to facilitate nickel-catalyzed cross-coupling reactions.

Angewandte Chemie, International Edition published new progress about 138429-17-1. 138429-17-1 belongs to oxazolidine, auxiliary class BOX Ligands, name is (4S,4’S)-4,4′-Diisobutyl-4,4′,5,5′-tetrahydro-2,2′-bioxazole, and the molecular formula is C14H24N2O2, Application of (4S,4’S)-4,4′-Diisobutyl-4,4′,5,5′-tetrahydro-2,2′-bioxazole.

Referemce:
https://en.wikipedia.org/wiki/Oxazolidine,
Oxazolidine | C3H7NO – PubChem

Huang, Quan published the artcileTuning the dual emission of keto/enol forms of excited-state intramolecular proton transfer (ESIPT) emitters via intramolecular charge transfer (ICT), COA of Formula: C9H6BrNO, the publication is Dyes and Pigments (2021), 109497, database is CAplus.

Herein disclosed the adjustment of the dual emission of keto and enol forms of excited-state intramol. proton transfer (ESIPT) emitters via intramol. charge transfer (ICT) effects. Introducing electron-donating triphenylamine (TPA) and electron-withdrawing triphenylboron (TPB) substituents into the para-position of the phenolic hydroxyl group or the side of the oxazole of 2-(2′-hydroxyphenyl)oxazole skeleton endows the resulting compounds (6a-6d) with different photophys. properties. Owing to the ICT effect from electronic donor to acceptor, introducing TPA into the side of oxazole and TPB into the para-position of phenolic hydroxyl is conducive to an enol-form emission (6a). Exchanging the 2 substituents, introducing TPB into the side of oxazole and TPA into the para-position of phenolic hydroxyl, would be beneficial to a keto-form emission (6b). Synchronously introducing 2 identical substituents, whether TPA or TPB, into 2 sides of 2-(2′-hydroxyphenyl)oxazole skeleton (6c and 6d) would lead to the dual emission of keto and enol forms due to the excited-state equilibrium of ESIPT reactions, which are further verified by DFT calculation The organic light-emitting diode (OLED) devices with 6a and 6c as emitters were fabricated, both of which exhibit hybridized local and charge transfer (HLCT) excited-state characters with high external quantum efficiencies (EQEs) of 4.9% and 5.6%, resp.

Dyes and Pigments published new progress about 72571-06-3. 72571-06-3 belongs to oxazolidine, auxiliary class Oxazole,Bromide,Benzene, name is 5-(4-Bromophenyl)oxazole, and the molecular formula is C9H6BrNO, COA of Formula: C9H6BrNO.

Referemce:
https://en.wikipedia.org/wiki/Oxazolidine,
Oxazolidine | C3H7NO – PubChem

Ames, Jennifer M. published the artcileEffect of pH, Temperature, and Moisture on the Formation of Volatile Compounds in Glycine/Glucose Model Systems, Category: oxazolidine, the publication is Journal of Agricultural and Food Chemistry (2001), 49(9), 4315-4323, database is CAplus and MEDLINE.

Mixtures of glycine, glucose, and starch were extrusion cooked using sodium hydroxide at 0, 3, and 6 g/L of extruder water feed, 18% moisture, and 120, 150, and 180 °C target die temperatures, giving extrudates with pH values of 5.6, 6.8, and 7.4. Freeze-dried equimolar solutions of glucose and glycine were heated either dry or after equilibration to �3% moisture at 180°C in a reaction-tube system designed to mimic the heating profile in an extruder. Volatile compounds were isolated onto Tenax and analyzed by gas chromatog.-mass spectrometry. For the extrudates, total yields of volatiles increased with decreasing pH at 180°C, reached a maximum at pH 6.8 at 150°C, and increased with increasing pH at 120°C. Amounts increased with temperature at all pH values. Pyrazines were the most abundant class for all sets of conditions (54-79% of total volatiles). Pyrroles, ketones, furans, oxazoles, and pyridines were also identified. Yields of volatiles from the reaction-tube samples increased by >60% in the moist system. Levels of individual classes also increased in the presence of moisture, except pyrazines, which decreased �.5-fold. Twenty-one of the compounds were common to the reaction-tube samples and the extrudates.

Journal of Agricultural and Food Chemistry published new progress about 20662-83-3. 20662-83-3 belongs to oxazolidine, auxiliary class Oxazole, name is 4,5-Dimethyloxazole, and the molecular formula is C5H7NO, Category: oxazolidine.

Referemce:
https://en.wikipedia.org/wiki/Oxazolidine,
Oxazolidine | C3H7NO – PubChem

Ames, Jennifer M. published the artcileEffect of pH and Temperature on the Formation of Volatile Compounds in Cysteine/Reducing Sugar/Starch Mixtures during Extrusion Cooking, HPLC of Formula: 20662-83-3, the publication is Journal of Agricultural and Food Chemistry (2001), 49(4), 1885-1894, database is CAplus and MEDLINE.

Mixtures of cysteine, reducing sugar (xylose or glucose), and starch were extrusion cooked using feed pH values of 5.5, 6.5, and 7.5 and target die temperatures of 120, 150, and 180 °C. Volatile compounds were isolated by headspace trapping onto Tenax and analyzed by gas chromatog.-mass spectrometry. Eighty and 38 compounds, resp., were identified from extrudates prepared using glucose and xylose. Amounts of most compounds increased with temperature and pH. Aliphatic sulfur compounds, thiophenes, pyrazines, and thiazoles were the most abundant chem. classes for the glucose samples, whereas for xylose extrudates highest levels were obtained for non-sulfur-containing furans, thiophenes, sulfur-containing furans, and pyrazines. 2-Furanmethanethiol and 2-methyl-3-furanthiol were present in extrudates prepared using both sugars, but levels were higher in xylose samples. The profiles of reaction products were different from those obtained from aqueous or reduced-moisture systems based on cysteine and either glucose or ribose.

Journal of Agricultural and Food Chemistry published new progress about 20662-83-3. 20662-83-3 belongs to oxazolidine, auxiliary class Oxazole, name is 4,5-Dimethyloxazole, and the molecular formula is C5H7NO, HPLC of Formula: 20662-83-3.

Referemce:
https://en.wikipedia.org/wiki/Oxazolidine,
Oxazolidine | C3H7NO – PubChem

Yaylayan, Varoujan A. published the artcileMechanism of imidazole and oxazole formation in [¹³C-2]-labelled glycine and alanine model systems, Category: oxazolidine, the publication is Food Chemistry (2003), 81(3), 403-409, database is CAplus.

Studies with ¹³C-2-labeled glycine and alanine in model systems containing 2,3-butanedione, glyceraldehyde or glyoxal have indicated that imidazoles and oxazoles can be formed from α-dicarbonyl compounds through Strecker reaction and subsequent formation of α-amino carbonyl reactive intermediates. These intermediates can react with any aldehyde in the reaction mixture to form an imine which in turn can either cyclize to form oxazoles or react with an amino compound and then cyclize to form imidazole after an oxidation step. On the other hand, Amadori products, formed in α-hydroxycarbonyl containing systems, can undergo decarboxylation followed by reaction with ammonia to form an amino imine intermediate which, after reaction with any aldehyde followed by cyclization, can form imidazoles after a dehydration step. This latter mechanism fixes the C-2 atom of glycine as an N-alkyl substituent in imidazoles. In addition, model studies with α-dicarbonyl compounds, using ammonium carbonate as a source of ammonia and paraformaldehyde as a source of formaldehyde, also produced imidazoles and oxazoles.

Food Chemistry published new progress about 20662-83-3. 20662-83-3 belongs to oxazolidine, auxiliary class Oxazole, name is 4,5-Dimethyloxazole, and the molecular formula is C5H8N2O, Category: oxazolidine.

Referemce:
https://en.wikipedia.org/wiki/Oxazolidine,
Oxazolidine | C3H7NO – PubChem

Lu, Chih-ying published the artcileEffects of water content on volatile generation and peptide degradation in the Maillard reaction of glycine, diglycine, and triglycine, Safety of 4,5-Dimethyloxazole, the publication is Journal of Agricultural and Food Chemistry (2005), 53(16), 6443-6447, database is CAplus and MEDLINE.

Peptides abundant in food and protein hydrolyzates are known to be important to process flavors. The present study reports the volatile profile of the Maillard reactions of glycine, diglycine, and triglycine. The reaction with glucose was conducted at 0-100% water content in glycerol medium at 160° for 1 h. Volatile compounds were quantified by stir bar sorptive extraction-gas chromatog.-mass spectrometry, and nonvolatile compounds were quantified by high-performance liquid chromatog.-tandem mass spectrometry. The major volatiles produced from each of the reaction systems were trimethylpyrazine and 2,5-dimethylpyrazine. Volatile generation increased as water decreased, and the overall reactivity of the glycine and glycine peptides in volatile formation was glycine â‰?triglycine > diglycine. Triglycine was very unstable and mainly degraded into cyclic Gly-Gly and glycine, whereas diglycine had a higher stability than triglycine toward hydrolytic cleavage of the peptide bond. The amounts of glycine, diglycine, cyclic (Gly-Gly), and triglycine in the peptide-glucose reaction mixtures at different water content were reported.

Journal of Agricultural and Food Chemistry published new progress about 20662-83-3. 20662-83-3 belongs to oxazolidine, auxiliary class Oxazole, name is 4,5-Dimethyloxazole, and the molecular formula is C5H7NO, Safety of 4,5-Dimethyloxazole.

Referemce:
https://en.wikipedia.org/wiki/Oxazolidine,
Oxazolidine | C3H7NO – PubChem

Kubota, Etsuro published the artcileOxazoles and pyrazines identified in roasted green tea aroma, Recommanded Product: 4,5-Dimethyloxazole, the publication is Chagyo Gijutsu Kenkyu (1983), 59-61, database is CAplus.

From the basis fraction of roasted green tea, 2 oxazoles, 14 alkylpyrazines, 3 cyclopentapyrazines, and 4 furan compounds were separated The 2 oxazoles were identified as 4,5-dimethyloxazole  [20662-83-3] and 2,4,5-trimethyloxazole  [20662-84-4] by gas chromatog.-mass spectrometry. Alkylpyrazines constituted �0% of the volatiles in the basic fraction.

Chagyo Gijutsu Kenkyu published new progress about 20662-83-3. 20662-83-3 belongs to oxazolidine, auxiliary class Oxazole, name is 4,5-Dimethyloxazole, and the molecular formula is C5H7NO, Recommanded Product: 4,5-Dimethyloxazole.

Referemce:
https://en.wikipedia.org/wiki/Oxazolidine,
Oxazolidine | C3H7NO – PubChem