Heterocyclic Building Blocks-Oxazolidine

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

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

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

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

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

Duppeti, Haritha published the artcileInfluence of processing conditions on the aroma profile of Litopenaeus vannamei by SPME-GC-MS, Formula: C5H7NO, the publication is Flavour and Fragrance Journal, database is CAplus.

This study reports the aroma profile of Litopenaeus vannamei under different processing conditions such as raw, boiled, hot air dried, microwave dried and roasted using SPME-GC-MS. A total of 86 volatile compounds were identified, among which 38 compounds reported as aroma-active compounds (AAC) having the odor activity value (OAV) greater than one. The microwave-dried shrimp meat (MSM) exhibited the highest summation of odor activity value, and roasted shrimp meat (RSM) showed the highest concentration of aroma-active compounds (3448.78 μg/g). The partial least square regression (PLSR) anal. and cluster anal. (CA) showed that MSM and RSM are related to each other in their aroma characteristics while boiled shrimp meat (BSM) is different than these samples. The results of this study illustrate the typical volatile markers and the impact of processing methods on flavor generation in L. vannamei, which should be examined for the assessment of its freshness and product development based on shrimp flavor.

Flavour and Fragrance Journal 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

Joshi, Poorvashree published the artcileUnlocking the concealed targets using system biology mapping for Alzheimer′s disease, COA of Formula: C14H17FN4O3, the publication is Pharmacological Reports (2019), 71(6), 1104-1107, database is CAplus and MEDLINE.

Alzheimer′s disease (AD) constitutes a neural loss in histol. of brain with involvement of complex genomic and environmental factors. Accumulation of amyloid beta (Aβ) peptide and phosphorylated tau are indicative of progression and cognitive decline. Hence an understanding of the underlying biol. pathways and targets along with associated mechanisms would be useful for the development of improved therapeutics for treating AD. In the present work, we aim to identify concealed targets for developing first line therapeutics and repositioning of validated targets as well as FDA- approved drugs using a system biol. approach. We have collated information pertaining to the biol. targets as well as the approved drugs, from scientific literature and patents. In all, the imbalance in the functioning of around 79 proteins and genes were identified to be involved in Alzheimer′s cascade. Amongst them, around 21 targets were found to be under therapeutic consideration for AD. Of the remaining, around 17 targets were reported as potential targets for AD, although they are under researcher′s attention for other physio-pathol. conditions. The anal. further revealed that âˆ?1 therapeutic targets are pharmacol. concealed but structurally validated targets and may constitute as potential therapeutic candidate for future drug discovery for AD.The biol. pathway vs. drug mapping provides a complete overview about underlying biol. pathways, therapeutic targets (explored and concealed), associated mechanisms, existing therapeutics and the information pertaining to mols. currently under active drug development for further drug discovery and drug re-positioning/repurposing approaches for AD management.

Pharmacological Reports 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, COA of Formula: C14H17FN4O3.

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

Savanur, Hemantkumar M. published the artcileLibraries of C-5 Substituted Imidazoles and Oxazoles by Sequential Van Leusen (VL)-Suzuki, VL-Heck and VL-Sonogashira in Imidazolium-ILs with Piperidine-Appended-IL as Base, Safety of 5-(4-Bromophenyl)oxazole, the publication is European Journal of Organic Chemistry (2018), 2018(38), 5285-5288, database is CAplus.

Facile access to diverse C5-substituted imidazoles and oxazoles via sequential Van Leusen-Suzuki, Van Leusen-Heck, and Van Leusen-Sonogashira protocols, employing imidazolium-ILs as solvents along with piperidine-appended imidazolium [PAIM][NTf₂] as task-specific basic IL has been demonstrated, in a high-yielding one-pot method, starting with readily available aldimines (for imidazole) or aldehydes (for oxazole) and tosylmethyl isocyanide (TOSMIC), under mild conditions with potential for recycling and reuse of the IL solvent. The scope of the method is supported 49 examples.

European Journal of Organic Chemistry 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, Safety of 5-(4-Bromophenyl)oxazole.

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

Jeong, Ji-Woong published the artcileIn vitro and in vivo activities of LCB01-0371, a new oxazolidinone, Quality Control of 1219707-39-7, the publication is Antimicrobial Agents and Chemotherapy (2010), 54(12), 5359-5362, database is CAplus and MEDLINE.

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

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, Quality Control of 1219707-39-7.

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

Zong, Zhaojing published the artcileComparison of In Vitro activity and MIC distributions between the novel oxazolidinone delpazolid and linezolid against multidrug-resistant and extensively drug-resistant Mycobacterium tuberculosis in China, Related Products of oxazolidine, the publication is Antimicrobial Agents and Chemotherapy (2018), 62(8), e00165-18/1-e00165-18/8, database is CAplus and MEDLINE.

Oxazolidinones are efficacious in treating mycobacterial infections, including tuberculosis (TB) caused by drug-resistant Mycobacterium tuberculosis. In this study, we compared the in vitro activities and MIC distributions of delpazolid, a novel oxazolidinone, and linezolid against multidrug-resistant TB (MDR-TB) and extensively drug-resistant TB (XDR-TB) in China. Addnl., genetic mutations in 23S rRNA, rplC, and rplD genes were analyzed to reveal potential mechanisms underlying the observed oxazolidinone resistance. A total of 240 M. tuberculosis isolates were included in this study, including 120 MDR-TB isolates and 120 XDR-TB isolates. Overall, linezolid and delpazolid MIC₉₀ values for M. tuberculosis isolates were 0.25 mg/L and 0.5 mg/L, resp. Based on visual inspection, we tentatively set epidemiol. cutoff (ECOFF) values for MIC determinations for linezolid and delpazolid at 1.0 mg/L and 2.0 mg/L, resp. Although no significant difference in resistance rates was observed between linezolid and delpazolid among XDR-TB isolates (P > 0.05), statistical anal. revealed a significantly greater proportion of linezolidresistant isolates than delpazolid-resistant isolates within the MDR-TB group (P = 0.036). Seven (53.85%) of 13 linezolid-resistant isolates were found to harbor mutations within the three target genes. Addnl., 1 isolate exhibited an amino acid substitution (Arg126His) within the protein encoded by rplD that contributed to high-level resistance to linezolid (MIC of >16 mg/L), compared to a delpazolid MIC of 0.25. In conclusion, in vitro susceptibility testing revealed that delpazolid antibacterial activity was comparable to that of linezolid. A novel mutation within rplD that endowed M. tuberculosis with linezolid, but not delpazolid, resistance was identified.

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 C37H30ClIrOP2, Related Products of oxazolidine.

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