Day: November 21, 2022

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

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

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 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

Wang, Min published the artcileA highly efficient palladium-catalyzed desulfitative arylation of azoles with sodium arylsulfinates, Name: 5-(4-Bromophenyl)oxazole, the publication is Tetrahedron (2012), 68(7), 1926-1930, database is CAplus.

A highly efficient palladium-catalyzed direct desulfitative arylation of azoles at C2-position has been developed using sodium arylsulfinates as aryl sources. Azoles including benzoxazoles, benzothiazoles, oxazoles, thiazoles, and 1,3,4-oxadiazoles reacted with sodium arylsulfinates smoothly to generate the corresponding products in good to excellent yields, and various substitution patterns were tolerated toward the reaction.

Tetrahedron 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 C8H17Br, Name: 5-(4-Bromophenyl)oxazole.

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

Alzieu, Thibaut published the artcileConverting oxazoles into imidazoles: new opportunities for diversity-oriented synthesis, Quality Control of 72571-06-3, the publication is Chemical Communications (Cambridge, United Kingdom) (2014), 50(15), 1867-1870, database is CAplus and MEDLINE.

We report the optimization of a neglected reaction for the rapid and direct conversion of oxazoles into N-substituted imidazoles. The utility of this microwave-promoted reaction for diversity-oriented synthesis is demonstrated in the preparation of >40 N-substituted imidazoles, including α-imidazolyl esters.

Chemical Communications (Cambridge, United Kingdom) 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, Quality Control of 72571-06-3.

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

Lee, Hyun-Hee published the artcileResistance mechanism of Enterococcus faecalis to LCB01-0371, a new oxazolidinone, Application 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 Yakhak Hoechi (2014), 58(1), 7-11, database is CAplus.

To study the resistance mechanism of E. faecalis to LCB01-0371, several resistant mutants to LCB01-0371 or linezolid were isolated by step-wise selection. The frequency of spontaneous mutations resistant to LCB01-0371 was lower than that of linezolid in E. faecalis. The genetic variations in resistant mutants were analyzed by DNA sequencing of domain V of 23S rRNA in each mutant. The first-step mutant to LCB01-0371 had a G2576T point mutation in V domain of 23S rRNA. However, no resistant mutant to LCB01-0371 was isolated in second-step mutant selection.

Yakhak Hoechi 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, Application 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

Choi, Yewon published the artcileSafety, tolerability and pharmacokinetics of 21 day multiple oral administration of a new oxazolidinone antibiotic, LCB01-0371, in healthy male subjects, Related Products of oxazolidine, the publication is Journal of Antimicrobial Chemotherapy (2018), 73(1), 183-190, database is CAplus and MEDLINE.

Background: LCB01-0371 is a new oxazolidinone antibiotic, which targets most Gram-pos. organisms. High rates of adverse reactions including myelosuppression have been reported for existing oxazolidinones, limiting their long-term use. Objectives: The safety, tolerability and pharmacokinetics (PK) of 21 day multiple oral administrations of LCB01-0371 in healthy male subjects (clinicaltrials.gov: NCT02540460) were investigated. Methods: In this randomized, double-blind, placebo-controlled study, subjects received 800mg of LCB01-0371 once or twice daily or 1200mg of LCB01-0371 twice-daily for 21 days in a fasting state. Safety and tolerability profiles including laboratory tests were evaluated during the study and on a post-study visit and the results were analyzed using repeated-measures anal. of variance (RM-ANOVA). Serial blood samples for PK anal. were collected up to 12 h after dosing on day 21. Results: A total of 40 subjects were enrolled and 34 subjects completed the study. Two subjects dropped out according to stopping rules. In the 1200mg twice-daily dose group, the absolute value of red blood cell count, haematocrit and Hb decreased by 500×10⁶/L (6.5%), 4.5% (6.8%) and 1.6 g/dL (6.9%), resp., after 21 day administrations of LCB01-0371. However, mean relative changes from baseline of all haematol. values were not significantly different among doses, including placebo (all, P<0.05). PK profiles of LCB01-0371 in the dose range of 800mg once daily to 1200mg twice daily were consistent with previous studies. Conclusions: LCB01-0371 is well tolerated in healthy male subjects with comparable haematol. profiles to placebo, after multiple doses of up to 1200mg twice daily for 21 days.

Journal of Antimicrobial 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, Related Products of oxazolidine.

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

Ho, Chi Tang published the artcileIsolation and identification of volatile flavor compounds in fried bacon, Computed Properties of 20662-83-3, the publication is Journal of Agricultural and Food Chemistry (1983), 31(2), 336-42, database is CAplus.

Volatile flavor compounds were isolated from 120 lb of fried bacon by a specially designed apparatus The isolated volatile flavor compounds were subjected to extensive gas chromatog. fractionation, and the pure fractions obtained were identified by IR and mass spectrometry. A total of 135 compounds were identified. The compounds identified in the volatiles of fried bacon included hydrocarbons, alcs., ketones, aldehydes, acids, esters, ethers, phenols, pyrazines, furans, thiazoles, oxazoles, oxazolines, pyrroles, pyridines, and miscellaneous compounds Two interesting halogenated pyrroles, N-acetyl-2-chloropyrrole  [84455-05-0] and N-acetyl-2-bromopyrrole  [84455-06-1], were synthesized to confirm the identification.

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, Computed Properties of 20662-83-3.

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

Carlin, James T. published the artcileComparison of acidic and basic volatile compounds of cocoa butters from roasted and unroasted cocoa beans, Formula: C5H7NO, the publication is JAOCS, J. Am. Oil Chem. Soc. (1986), 63(8), 1031-6, database is CAplus.

A total of 9 acidic and 83 basic compounds was identified in the roasted and unroasted cocoa butter samples. Forty-seven of the compounds identified are reported for the 1st time in cocoa. The higher concentration of short-chain fatty acids in the unroasted cocoa butter is responsible for its acidic aroma characteristics. The roasted cocoa butter generally contained greater numbers and higher concentrations of compounds whose formations would be favored by thermal processing. These compounds included pyrazines, thiazoles, oxazoles, and pyridines. The aromas of many of these compounds are characteristic of the aroma differences between the 2 cocoa butters and contribute to the cocoa aroma of roasted cocoa butter.

JAOCS, J. Am. Oil Chem. Soc. 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, Formula: C5H7NO.

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