Day: November 21, 2022

Chen, Wei published the artcileEffects of parecoxib sodium preemptive analgesia on postoperative inflammatory cytokines and stress responses in elderly patients undergoing total hip replacement, COA of Formula: C19H17N2NaO4S, the publication is Huaxi Yixue (2015), 30(6), 1067-1070, database is CAplus.

Objective: To investigate whether parecoxib sodium preemptive analgesia reduces inflammatory cytokines and stress hormones production in elderly patients after total hip replacement. Methods: Sixty patients with American Society of Anesthesiologists Classification I-II undergoing total hip replacement for femoral neck fracture or aseptic necrosis of the femoral head, aged between 60 and 90 years with a body weight more than 50 kg, were randomly divided into preemptive analgesia group (group P, n = 30) and control group (group C, n = 30). The patients in group P received parecoxib sodium 40 mg i.v. 30 min before skin incision, and another 20 mg 8 h after the first administration. All the patients in the two groups received the administration of patient-controlled analgesia sufentanyl. We recorded blood levels of interleukin-6 (IL-6), tumor necrosis factor alpha (TNF-α), cortisol (COR), adrenaline (AD) and noradrenaline (NAD) 30 min before skin incision, and 1 h, 6 h, 12 h and 24 h postoperatively. Results: The blood levels of IL-6, TNF-α, COR, AD and NAD in group P at 1 h, 6 h, 12 h or 24 h postoperatively were significantly lower than those in group C (P<0.05). Conclusion: Parecoxib sodium preemptive analgesia reduces postoperative inflammatory cytokines and stress hormones production in elderly patients undergoing total hip replacement.

Huaxi Yixue published new progress about 198470-85-8. 198470-85-8 belongs to isoxazole, auxiliary class Immunology/Inflammation,COX, name is Sodium ((4-(5-methyl-3-phenylisoxazol-4-yl)phenyl)sulfonyl)(propionyl)amide, and the molecular formula is C19H17N2NaO4S, COA of Formula: C19H17N2NaO4S.

Referemce:
https://en.wikipedia.org/wiki/Isoxazole,
Isoxazole | C3H3NO – PubChem

Li, Hai-ying published the artcileEffect of ulinastatin and parecoxib sodium on intrapulmonary shunt fraction during one lung ventilation, SDS of cas: 198470-85-8, the publication is Shiyong Yaowu Yu Linchuang (2017), 20(1), 30-34, database is CAplus.

Objective: To explore the effect of ulinastatin and parecoxib sodium on intrapulmonary shunt during one lung ventilation. Methods: One hundred patients receiving one lung ventilation treatment for esophageal cancer from Apr. 2014 to Apr. 2015 were involved as the observation objects. According to the patient preference, patients were divided into group A (n=50) and group B (n=50). The same induction of anesthesia and anesthesia drugs were given to them to maintain the same depth of anesthesia. Half an hour before anesthesia, 40 mg parecoxib sodium was given to group A, and 50 U UTI was given to group B. The mean airway pressure, heart rate, mean arterial pressure, oxygen saturation, arterial carbon dioxide partial pressure, pulmonary shunt fraction, interleukin (IL)-6, IL-8 Junior necrosis factor α and C-protein expression were compared at the following time points: after induction of anesthesia (S₁ period), 0.5 h after one-Lung ventilation (S₂ period), 1 h after one lung ventilation (S₃ period) and 0.5 h after restoring lung ventilation (S₄ period). Results: The mean arterial pressure of group A (77.9±11.5) was higher than that of group B (73.6±9.1) at the period of S₄, the difference was statistically significant (P<0.05). The arterial carbon dioxide tension of group A (41.4±3.8, 41.8±3.4, 41.7±2.8) was higher than that of group B (42.7±2.1, 42.7±2.1, 44.8±3.7) at the period of S₂, S₃ and S₄, the difference were statistically significant (P<0.05). The pulmonary shunt fraction of group A was lower than that of group B on the period of S₂ and S₃. The pulmonary shunt fractions of the two groups on the period of S₂ and S₃ were higher than those on the period of S₄. Conclusion: Parecoxib sodium and ulinastatin have protective effect on one lung ventilation, but parecoxib sodium reduces intrapulmonary shunt fraction more significantly which can avoid the damage to the lung tissue to some extent.

Shiyong Yaowu Yu Linchuang published new progress about 198470-85-8. 198470-85-8 belongs to isoxazole, auxiliary class Immunology/Inflammation,COX, name is Sodium ((4-(5-methyl-3-phenylisoxazol-4-yl)phenyl)sulfonyl)(propionyl)amide, and the molecular formula is C19H17N2NaO4S, SDS of cas: 198470-85-8.

Referemce:
https://en.wikipedia.org/wiki/Isoxazole,
Isoxazole | C3H3NO – PubChem

Wang, Afang published the artcileRetrospective analysis on the inhibiting effect of parecoxib sodium on the inflammatory factors and stress response in patients after hip and knee replacement surgery, Formula: C19H17N2NaO4S, the publication is Yaowu Liuxingbingxue Zazhi (2016), 25(3), 146-149, database is CAplus.

Objective: To evaluate the stress reaction and inflammatory factor inhibition effect of parecoxib sodium continuous pumped after hip and knee arthroplasty, and provide a reference for the orthopaedic perioperative analgesic solution Methods: 52 cases of total hip, semi hip and knee joint surface replacement patientsâ€?clin. data were retrospectively analyzed, which divided into observation group and control group according to analgesic method, 26 cases in each group. The control group received bupivacaine for patient controlled epidural analgesia therapy after operation, patients in the observation group combined with parecoxib sodium i.v. injection pumped, 5 mg per h. The level of pain relief in different time points were observed The levels of plasma inflammatory factor, cortisol (Cor), and adrenocorticotropic hormone (Glu) were compared in the two groups. Results: The VAS score of observation group was lower than that of the control group in every time points (P<0.05). The 0 and I pain levels of IL-6 and IL-1β in the observation group were significantly higher than those in the control group (P>0.05). The levels of IL-6 and IL-1β were significantly different between two groups (Glu), and the levels of Cor and Glu were significantly lower in two groups (P<0.05). The index level of observation group were significantly lower than the control group (P<0.05). Conclusion: Parecoxib sodium continuous pumped could alleviate the pain of hip and knee replacement in patients with postoperative, reduce the levels of inflammatory factors and stress level, it was worth clin. promotion.

Yaowu Liuxingbingxue Zazhi published new progress about 198470-85-8. 198470-85-8 belongs to isoxazole, auxiliary class Immunology/Inflammation,COX, name is Sodium ((4-(5-methyl-3-phenylisoxazol-4-yl)phenyl)sulfonyl)(propionyl)amide, and the molecular formula is C8H11BO2, Formula: C19H17N2NaO4S.

Referemce:
https://en.wikipedia.org/wiki/Isoxazole,
Isoxazole | C3H3NO – PubChem

Luo, Si-jia published the artcileEffect of oxycodone combined with parecoxib sodium on pain relief after laparoscopic cholecystectomy, Recommanded Product: Sodium ((4-(5-methyl-3-phenylisoxazol-4-yl)phenyl)sulfonyl)(propionyl)amide, the publication is Zhongguo Xiandai Putong Waike Jinzhan (2017), 20(10), 814-815, 818, database is CAplus.

To explore the safety of oxycodone combined with parecoxib sodium in laparoscopic cholecystectomy. According to the random number table method, 102 patients who were to undergo laparoscopic cholecystectomy were divided into a control group and an observation group, with 51 cases in each group. The control group was anesthetized with morphine combined with parecoxib sodium. The observation group was anesthetized with oxycodone combined with parecoxib sodium. The pain conditions of the two groups of patients were evaluated at 3, 12, 24, and 48 h after the operation, and the number of PCA compressions and the addnl. analgesics in the two groups within 48 h after the operation were recorded. At 3, 12, 24, and 48 h after surgery, the difference in pain scores during resting and coughing between the two groups was statistically significant (P < 0.05). The number of effective PCA compressions and the addnl. rate of analgesic drugs in the observation group within 48 h after surgery were significantly lower than those in the control group (P < 0.05). The incidence of adverse reactions in the observation group was 11.8%, which was significantly lower than the 37.3% in the control group (P < 0.05). During laparoscopic cholecystectomy, the use of oxycodone combined with parecoxib sodium anesthesia can not only achieve better anesthesia and analgesia, but also reduce the occurrence of adverse reactions, thereby ensuring the safety of patients.

Zhongguo Xiandai Putong Waike Jinzhan published new progress about 198470-85-8. 198470-85-8 belongs to isoxazole, auxiliary class Immunology/Inflammation,COX, name is Sodium ((4-(5-methyl-3-phenylisoxazol-4-yl)phenyl)sulfonyl)(propionyl)amide, and the molecular formula is C19H17N2NaO4S, Recommanded Product: Sodium ((4-(5-methyl-3-phenylisoxazol-4-yl)phenyl)sulfonyl)(propionyl)amide.

Referemce:
https://en.wikipedia.org/wiki/Isoxazole,
Isoxazole | C3H3NO – PubChem

Treitler, Daniel S. published the artcileDevelopment and Demonstration of a Safer Protocol for the Synthesis of 5-Aryltetrazoles from Aryl Nitriles, Related Products of isoxazole, the publication is Organic Process Research & Development (2017), 21(3), 460-467, database is CAplus.

The search for a faster, safer protocol for the direct synthesis of 5-aryltetrazoles from aryl nitriles in the presence of sodium azide and an amine hydrochloride salt led to the discovery of a buffered system comprised of BnNH₂, BnNH₂·HCl, and NaN₃. After optimization of reaction conditions and a thorough study of reaction safety, the procedure was demonstrated for the synthesis of several hundred grams of 4-chloro-2-(2H-tetrazol-5-yl)phenol. The generality of the developed reaction conditions was established by a small-scale reactivity screen using 16 addnl. aryl and heteroaryl nitrile substrates.

Organic Process Research & Development published new progress about 2251-79-8. 2251-79-8 belongs to isoxazole, auxiliary class Trifluoromethyl,Fluoride,Benzene, name is 5-(4-(Trifluoromethyl)phenyl)-1H-tetrazole, and the molecular formula is C8H16O2, Related Products of isoxazole.

Referemce:
https://en.wikipedia.org/wiki/Isoxazole,
Isoxazole | C3H3NO – PubChem

Martinez-Pardo, Pablo published the artcileEnantioselective Synthesis of Functionalized Diazaspirocycles from 4-Benzylideneisoxazol-5(4H)-one Derivatives and Isocyanoacetate Esters, Recommanded Product: 3-Phenylisoxazol-5(2H)-one, the publication is Advanced Synthesis & Catalysis (2020), 362(17), 3564-3569, database is CAplus.

Enantioenriched spirocyclic compounds bearing three contiguous stereocenters and high functionalization were obtained through a formal [3+2] cycloaddition reaction catalyzed by a cooperative system. The spiro compounds were synthesized from 4-arylideneisoxazol-5-ones and isocyanoacetate esters using a bifunctional squaramide/Bronsted base organocatalyst derived from a Cinchona alkaloid and silver oxide as Lewis acid. This method afforded two out of the four possible diastereomers with good yields and high enantiomeric excess for both diastereomers.

Advanced Synthesis & Catalysis published new progress about 1076-59-1. 1076-59-1 belongs to isoxazole, auxiliary class Oxazoline,Benzene,Ester, name is 3-Phenylisoxazol-5(2H)-one, and the molecular formula is C9H7NO2, Recommanded Product: 3-Phenylisoxazol-5(2H)-one.

Referemce:
https://en.wikipedia.org/wiki/Isoxazole,
Isoxazole | C3H3NO – PubChem

Sutariya, Tushar R. published the artcileA domino synthetic approach for new, angular pyrazol- and isoxazol-heterocycles using [DBU][Ac] as an effective reaction medium, Quality Control of 1076-59-1, the publication is RSC Advances (2015), 5(30), 23519-23529, database is CAplus.

The synthesis of pyrazole and isoxazole based heterocycles, e.g., I and II (R = H, Cl), via domino Knoevenagel-hetero-Diels-Alder (DKHDA) reaction of O-alkenylated acetophenones with active methylene pyrazolones and 3-phenyl-1,2-oxazol-5-one, resp., in an ionic liquid [DBU][Ac], effectively at 130 °C were described. The DKHDA reaction of O-alkynylated acetophenones is also feasible with 3-phenyl-1,2-oxazol-5-one but in the presence of ZnO as catalyst because it contains the unactivated dienophile moiety. The heterosteroid-mimicking structure II (R = H, Cl) thus achieved may have different bioprofiles than the aldehyde-derived one. The use of recyclable ionic liquid in place of organic solvents in the present method offers both ecol. and environmental benefits. The stereochem. of synthesized compounds was confirmed by the single crystal X-ray diffraction data.

RSC Advances published new progress about 1076-59-1. 1076-59-1 belongs to isoxazole, auxiliary class Oxazoline,Benzene,Ester, name is 3-Phenylisoxazol-5(2H)-one, and the molecular formula is C9H11BO4, Quality Control of 1076-59-1.

Referemce:
https://en.wikipedia.org/wiki/Isoxazole,
Isoxazole | C3H3NO – PubChem

Aridoss, Gopalakrishnan published the artcileHighly Efficient Synthesis of 5-Substituted 1H-Tetrazoles Catalyzed by Cu-Zn Alloy Nanopowder, Conversion into 1,5- and 2,5-Disubstituted Tetrazoles, and Synthesis and NMR Studies of New Tetrazolium Ionic Liquids, SDS of cas: 2251-79-8, the publication is European Journal of Organic Chemistry (2011), 2011(31), 6343-6355, S6343/1-S6343/57, database is CAplus.

A series of 5-substituted 1H-tetrazoles were synthesized through [3+2] cycloaddition reactions between nitriles RCN and NaN₃ in the presence of Cu-Zn alloy nanopowder as catalyst. The 1,5-di-Bu, 1-butyl-5-hexyl, 2,5-di-Bu, and 2-butyl-5-hexyl derivatives were then used as building blocks to synthesize several novel tetrazolium ionic liquids (ILs) with EtSO₄^–, OTf^–, and NTf₂^– counterions. Whereas alkylation of the 2,5-dialkyltetrazoles selectively gave the N-4 alkylated onium salts, with the 1,5-dialkyl derivatives approx. 1:1 mixtures of two tetrazolium salts were formed by alkylation at N-3 and N-4. The triflate and Et sulfate salts are room-temperature ILs that are hydrophilic, whereas the NTf₂ salts are low-melting ILs and are hydrophobic. The resulting tetrazolium-based ionic liquids were studied by various multinuclear and 2D NMR techniques including natural abundance ¹⁵N and ¹H/¹⁵N correlations.

European Journal of Organic Chemistry published new progress about 2251-79-8. 2251-79-8 belongs to isoxazole, auxiliary class Trifluoromethyl,Fluoride,Benzene, name is 5-(4-(Trifluoromethyl)phenyl)-1H-tetrazole, and the molecular formula is C8H5F3N4, SDS of cas: 2251-79-8.

Referemce:
https://en.wikipedia.org/wiki/Isoxazole,
Isoxazole | C3H3NO – PubChem

Lee, Seungbeom published the artcileDiscovery of novel potent migrastatic Thiazolo[5,4-b]pyridines targeting Lysyl-tRNA synthetase (KRS) for treatment of Cancer metastasis, Application of 2-Chloro-5-nitrobenzoxazole, the publication is European Journal of Medicinal Chemistry (2021), 113405, database is CAplus and MEDLINE.

Recently, non-canonical roles of lysyl-tRNA synthetase (KRS), which is associated with cell migration and cancer metastasis, have been reported. Therefore, KRS has emerged as a promising target for the treatment of cell migration-related diseases, especially cancer metastasis, although the satisfying chem. inhibitors targeting KRS have not yet been identified. Here, we report the discovery of novel, mechanistically unique, and potent cell migration inhibitors targeting KRS, including the chem. and biol. studies on the most effective N,N-dialkylthiazolo[5,4-b]pyridin-2-amine (SL-1910, I). SL-1910 exhibited highly potent migration inhibition (EC₅₀ = 81 nM against the mutant KRS-overexpressed MDA-MB-231 cells) and was superior to the previously reported KRS inhibitor (migration inhibitory EC₅₀ = 8.5μM against H226 cells). The KRS protein binding study via fluorescence-based binding titration and KRS protein 2D-NMR mapping study, in vitro concentration-dependent cell migration inhibition, and in vivo anti-metastatic activity of SL-1910, which consists of a new scaffold, have been reported in this study. In addition, in vitro absorption, distribution, metabolism, and excretion studies and mouse pharmacokinetics experiments for SL-1910 were conducted.

European Journal of Medicinal Chemistry published new progress about 54120-91-1. 54120-91-1 belongs to isoxazole, auxiliary class Chloride,Nitro Compound,Benzooxazole, name is 2-Chloro-5-nitrobenzoxazole, and the molecular formula is C7H3ClN2O3, Application of 2-Chloro-5-nitrobenzoxazole.

Referemce:
https://en.wikipedia.org/wiki/Isoxazole,
Isoxazole | C3H3NO – PubChem

Nair, Satheesh published the artcileOptimization of Nicotinamides as Potent and Selective IRAK4 Inhibitors with Efficacy in a Murine Model of Psoriasis, Category: isoxazole, the publication is ACS Medicinal Chemistry Letters (2020), 11(7), 1402-1409, database is CAplus and MEDLINE.

IRAK4 is an attractive therapeutic target for the treatment of inflammatory conditions. Structure guided optimization of a nicotinamide series of inhibitors has been expanded to explore the IRAK4 front pocket. This has resulted in the identification of compounds such as 12 with improved potency and selectivity. Addnl. 12 demonstrated activity in a pharmacokinetics/pharmacodynamics (PK/PD) model. Further optimization efforts led to the identification of the highly kinome selective 21, which demonstrated a robust PD effect and efficacy in a TLR7 driven model of murine psoriasis.

ACS Medicinal Chemistry Letters published new progress about 874-36-2. 874-36-2 belongs to isoxazole, auxiliary class Other Aromatic Heterocyclic,Amine, name is Benzo[c][1,2,5]oxadiazol-5-amine, and the molecular formula is C6H5N3O, Category: isoxazole.

Referemce:
https://en.wikipedia.org/wiki/Isoxazole,
Isoxazole | C3H3NO – PubChem