Category: oxazolidine

Boger, Dale L. published the artcileDiscovery of a Potent, Selective, and Efficacious Class of Reversible α-Ketoheterocycle Inhibitors of Fatty Acid Amide Hydrolase Effective as Analgesics, Recommanded Product: 4,5-Dimethyloxazole, the publication is Journal of Medicinal Chemistry (2005), 48(6), 1849-1856, database is CAplus and MEDLINE.

Fatty acid amide hydrolase (FAAH) degrades neuromodulating fatty acid amides including anandamide (endogenous cannabinoid agonist) and oleamide (sleep-inducing lipid) at their sites of action and is intimately involved in their regulation. Herein the authors report the discovery of a potent, selective, and efficacious class of reversible FAAH inhibitors that produce analgesia in animal models validating a new therapeutic target for pain intervention. Key to the useful inhibitor discovery was the routine implementation of a proteomics-wide selectivity screen against the serine hydrolase superfamily ensuring selectivity for FAAH coupled with systematic in vivo examinations of candidate inhibitors.

Journal of Medicinal 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, Recommanded Product: 4,5-Dimethyloxazole.

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

Takahashi, K. published the artcileStructure of oxazolomycin, a new β-lactone antibiotic, Quality Control of 72571-06-3, the publication is Tennen Yuki Kagobutsu Toronkai Koen Yoshishu (1983), 189-96, database is CAplus.

Oxazolomycin (I) [89808-64-0] is a new antitumor antibiotic isolated from Streptomyces sp. (Y-32026). The structural elucidation of this noncrystalline antibiotic has been carried out. Its structure has been determined as I on the basis of spectral anal., x-ray crystallog. anal. and the synthesis of corresponding degraded products. The structure-biol. activity relationship was also studied. In vitro direct cytotoxicity of oxazole derivatives and each segment of oxazolomycin were examined

Tennen Yuki Kagobutsu Toronkai Koen Yoshishu 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 C6H12N2O, Quality Control of 72571-06-3.

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

Whitfield, Frank B. published the artcileHeterocyclic Volatiles Formed by Heating Cysteine or Hydrogen Sulfide with 4-Hydroxy-5-methyl-3(2H)-furanone at pH 6.5, SDS of cas: 20662-83-3, the publication is Journal of Agricultural and Food Chemistry (2001), 49(2), 816-822, database is CAplus and MEDLINE.

The reaction of 4-hydroxy-5-methyl-3(2H)-furanone (HMF) with cysteine or H₂S at pH 6.5 for 60 min at 140 °C produced complex mixtures of volatile compounds, the majority of these containing either sulfur or nitrogen. Of the 68 compounds detected, 63 were identified, some tentatively, by GC-MS. Among the identified compounds were thiophenes (10), thiophenones (6), thienothiophenes (5), thiazoles (5), trithiolanes (4), pyrazines (6), and oxazoles (4). More compounds were produced in the reaction of HMF with cysteine (63) than were formed in the reaction with hydrogen sulfide (33). In both systems, thiophenones were the major reaction products, accounting for 25-36% of the total volatiles formed. Possible reasons for the differences in the composition of the 2 systems are discussed. The contributions of these reactions, and their products, to the flavor of heated foods are considered.

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 C11H15NOS, SDS of cas: 20662-83-3.

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

Shimoda, Mitsuya published the artcileHeadspace gas analysis of volatile compounds of light and deep roasted sesame seed oil, Application In Synthesis of 20662-83-3, the publication is Food Science and Technology International, Tokyo (1998), 4(1), 14-17, database is CAplus.

Volatile compounds in the headspace gas of light and deep roasted sesame seed oil were analyzed by gas chromatog. and gas chromatog.-mass spectrometry. The present method resulted in good reproducibility (<6.6% as a relative standard deviation) in the determination of individual volatile components. About 64 compounds, including 30 heterocyclic compounds, 7 aliphatic aldehydes, 11 ketones, and 16 miscellaneous compounds, were identified. Peak area percentages of 2-methylpropanal, 2-butenal, 2- and 3-methylbutanal, 2-propanone, 2-butanone, 3-methyl-2-butanone, 2,3-butanedione, 2- and 3-methylfuran, and 2,5-dimethylfuran, all of which could not be detected by steam distillation and column adsorptive concentration (previous method), increased in deep roasted oil. Hexanal decreased from 6.13% to 2.55% in deep roasted oil. Compared with the previous method, pyridine, thiophenes, and sulfides could be detected only by the present method, but unsaturated aliphatic aldehydes could not.

Food Science and Technology International, Tokyo 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 C5H5ClO2, Application In Synthesis of 20662-83-3.

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

Tehrani, Kourosch Abbaspour published the artcileThermal Degradation Studies of Glucose/Glycine Melanoidins, Synthetic Route of 20662-83-3, the publication is Journal of Agricultural and Food Chemistry (2002), 50(14), 4062-4068, database is CAplus and MEDLINE.

Nondialyzable and water-insoluble melanoidins, isolated from a glucose/glycine model reaction mixture, which was prepared in a standardized way according to the guidelines of the COST Action 919, were heated at different temperatures ranging from 100 to 300 °C. Among the volatile compounds, which were analyzed by solid-phase microextraction and GC-MS, pyrazines, pyridines, pyrroles, and furans were detected. In general, total amounts of volatile compounds increased with the temperature When water-insoluble melanoidins were heated, especially at higher temperatures, this resulted in a higher diversity of isolated compounds For furans, pyrroles, pyrazines, and carbonyl compounds, a maximum was observed in the case of high mol. weight melanoidins around 200-220 °C. Pyridines and total oxazoles, however, were generated in higher yields with increasing temperatures Thus, the possibility of producing some flavor-significant volatiles from heated standard melanoidins at temperatures relevant to food preparation and contribute to the flavor aspects originating from melanoidins.

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 C10H14O2, Synthetic Route of 20662-83-3.

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

Kim, Ju Sang published the artcileEarly Bactericidal Activity of Delpazolid (LCB01-0371) in Patients with Pulmonary Tuberculosis., Category: oxazolidine, the publication is Antimicrobial agents and chemotherapy (2022), 66(2), e0168421, database is MEDLINE.

Delpazolid, an oxazolidinone, has been studied in non-clinical studies of efficacy and toxicity and Phase 1 clinical studies. Delpazolid has in vitro activity against Gram-positive bacteria, including Mycobacterium tuberculosis. This study evaluated the bactericidal activity, safety, and pharmacokinetics of delpazolid in patients with pulmonary tuberculosis (TB). Seventy-nine subjects, aged 19 to 75 years with newly diagnosed smear-positive TB with no prior treatment for the current episode and no confirmed resistance to rifampin or isoniazid, were randomized to receive delpazolid 800 mg once a day (QD), 400 mg twice a day (BID), 800 mg BID or 1,200 mg QD or an active control of isoniazid, rifampin, pyrazinamide, and ethambutol (HRZE) or linezolid 600 mg BID. The primary endpoint was the average daily reduction in log transformed bacterial load, assessed on 7H11 solid-media culture, from days 0 to 14. The average daily decline in log-CFU was 0.044 ±â€?.016, 0.053 ±â€?.017, 0.043 ±â€?.016, and 0.019 ±â€?.017, for the delpazolid 800 mg QD, 400 mg BID, 800 mg BID, and the 1,200 mg QD groups, respectively. The average daily decline in log-CFU was 0.192 ±â€?.028 for the HRZE group and 0.154 ±â€?.023 for the linezolid 600 mg BID group. Three serious adverse events (SAE) were reported, one each in the delpazolid 400 mg BID group (death due to worsening of TB at day 2), the HRZE group (hospitalization due to pleural effusion) and the linezolid group (hyperkalemia); none of the SAEs were assessed as related to study drugs. This study has been registered at ClinicalTrials.gov with registration number NCT02836483.

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, Category: oxazolidine.

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

Sunwoo, Jung published the artcileEffect of food on the pharmacokinetic characteristics of a single oral dose of LCB01-0371, a novel oxazolidinone antibiotic, HPLC of Formula: 1219707-39-7, the publication is Drug Design, Development and Therapy (2018), 1707-1714, database is CAplus and MEDLINE.

Background: LCB01-0371 is a novel oxazolidinone antibiotic that blocks protein production by binding to bacterial 23S ribosomes. This antibiotic is active against Gram-pos. bacteria. This study aimed to evaluate the effect of food on the pharmacokinetics (PKs) of LCB01-0371 and evaluate its safety profile. Subjects and methods: A randomized, open-label, two-way crossover study was performed in 18 healthy Korean male subjects. All subjects received a single oral 800 mg dose of LCB01-0371 in each period under fed or fasting condition with a 7-day washout in between. The fed condition was defined as consumption of a meal of 800-1,000 kcal containing �0% of fat content. Serial blood samples were collected over 24 h after dosing, and the PK parameters were calculated by noncompartment anal. All available data of the subjects who received LCB01-0371 at least once were included in the safety data summaries. Results: In the fed condition, both the maximum plasma concentration (Cmax) and the total systemic exposure (area under the plasma concentration-time curve from time zero to the last observed time point [AUClast]) decreased by �3% and 10%, resp. The time to reach Cmax was delayed by �.25 h in the fed condition, whereas the mean elimination half-life remained similar in both conditions. In the fed/fasting condition, the geometric mean ratios and 90% CI of the Cmax and AUClast were 0.666 (0.470-0.945) and 0.897 (0.761-1.057), resp. There were no drug-related adverse events (AEs) or serious AEs. Conclusion: Although the Tmax after a single oral 800 mg dose of LCB01-0371 was slightly delayed under the fed condition compared to the fasting condition, the total systemic exposure was similar under both conditions. Therefore, LCB01-0371 could be administered regardless of food intake.

Drug Design, Development and Therapy 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 C30H40N2O4, HPLC of Formula: 1219707-39-7.

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

Kameda, Minoru published the artcileOptimization of a series of 2,4-diaminopyridines as neuropeptide Y Y1 receptor antagonists with reduced hERG activity, COA of Formula: C5H7NO, the publication is Bioorganic & Medicinal Chemistry Letters (2009), 19(15), 4325-4329, database is CAplus and MEDLINE.

The synthesis and evaluation of a series of 2,4-diaminopyridine-based neuropeptide Y Y1 (NPY Y1) receptor antagonists are described. Compound I was previously reported by our laboratory to be a potent and selective Y1 antagonist; however, I was also found to have potent hERG inhibitory activity. The main focus of this communication is structure-activity relationship development aimed at eliminating the hERG activity of I. This resulted in the identification of compound II as a potent and selective NPY Y1 antagonist with reduced hERG liability.

Bioorganic & Medicinal Chemistry Letters 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, COA of Formula: C5H7NO.

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

Gollnick, Klaus published the artcile[4 + 2] Cycloaddition of singlet oxygen to oxazoles. Formation of oxazole endoperoxides, Related Products of oxazolidine, the publication is Tetrahedron Letters (1988), 29(9), 1003-6, database is CAplus.

Photochem. [4+2]-cycloaddition of singlet oxygen to oxazoles I (R, R¹, R² = H, Me, Ph) gave the endo peroxides II, which were isolated and characterized at low temperature 3-Methylisoxazole, 1,2,5-oxadiazoles and 1,3,4-oxadiazoles were inert to singlet oxygen under the same conditions.

Tetrahedron Letters 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, Related Products of oxazolidine.

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

Vercellotti, John R. published the artcileAnalysis of volatile heteroatomic meat flavor principles by purge-and-trap/gas chromatography-mass spectrometry, Formula: C5H7NO, the publication is Journal of Agricultural and Food Chemistry (1987), 35(6), 1030-5, database is CAplus.

A simple purge-and-trap/gas chromatog.-mass spectrometry (GC-MS) procedure was developed and proven effective for the comprehensive anal. of nitrogen-, oxygen-, and sulfur-containing volatile compounds in ground roast beef, com. beef flavor concentrate, and beef meat powder. GC was conducted on a 0.3 external diameter 50 m SE-54 (crosslinked 5% phenylmethylsilicone) column with He as carrier gas. These compounds, as released from the sample heated in the evaporator flask of a rotary evaporator, were effectively trapped in a Tenax-containing glass liner under 5 psi vacuum. The trap was then heated in an external inlet port, and the volatiles were purged into a GC-MS system for identification and concentration estimation More than 50 heteroat., mostly cyclic, compounds were identified in these samples.

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 C3H5F3O, Formula: C5H7NO.

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