Month: December 2022

Zhou, Kexu published the artcileCopper-catalyzed aerobic asymmetric cross-dehydrogenative coupling of C(sp³)-H bonds driven by visible light, Name: (3aS,3a’S,8aR,8a’R)-2,2′-(Cyclobutane-1,1-diyl)bis(3a,8a-dihydro-8H-indeno[1,2-d]oxazole), the publication is Green Chemistry (2020), 22(14), 4597-4603, database is CAplus.

A chiral-copper catalyst initiates the visible-light-driven oxidative CDC reaction by mol. oxygen, and governed the stereochem. In this way, a diastereo- and enantioselective synthesis of (imidazolyl)xanthenes such as I [R¹ = Me, Ph, Bn; R² = Me, cyclopropyl, Ph, etc.] via cross-dehydrogenative coupling between carbonyl compounds and xanthene derivatives was achieved. This work provided an economic and manageable approach to stereoselective C-C bond formation, and demonstrated a potential application of chiral copper catalysts in difficult asym. photochem. reactions.

Green Chemistry published new progress about 182122-10-7. 182122-10-7 belongs to isoxazole, auxiliary class BOX or PyBox,BOX or PyBox, name is (3aS,3a’S,8aR,8a’R)-2,2′-(Cyclobutane-1,1-diyl)bis(3a,8a-dihydro-8H-indeno[1,2-d]oxazole), and the molecular formula is C9H8BNO2, Name: (3aS,3a’S,8aR,8a’R)-2,2′-(Cyclobutane-1,1-diyl)bis(3a,8a-dihydro-8H-indeno[1,2-d]oxazole).

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

Cui, Wenyao published the artcileThe Study of Different Approaches of Parecoxib Sodium Pretreatment on the Behavior of Rats with Neuropathic Pain, Related Products of isoxazole, the publication is Cell Biochemistry and Biophysics (2015), 72(1), 137-140, database is CAplus and MEDLINE.

Our objective is to analyze and observe the different administration routes of parecoxib sodium pretreatment on the behavioral improvement of rats with neuropathic pain to provide the preclin. data of parecoxib sodium on neuropathic pain treatment. 30 SD rats were randomly divided into five groups, including model group, sham operation group, intrathecal injection group (IT group), i.p. injection group (IP group), and perineural infiltration group (PI group). The rats in model group and three parecoxib sodium pretreatment groups received spinal nerve ligation (SNL). Heat pain test and 50 % paw mech. withdrawal threshold test (50 % PMWT) were use to assess the responses after parecoxib sodium pretreatment. 50 % PMWT results of right foot in five groups had no statistical difference (P > 0.05); 50 % PMWT results of left and right feet in three parecoxib sodium pretreatment groups were obviously higher than SNL group at different time points, which was statistically different (P < 0.05); in comparison with three pretreatment groups, the data of left foot in IT group were obviously higher than PI group and IP group, and the comparison among three groups had significant difference (P < 0.05). However, the data of right foot had no significant difference among three groups (P > 0.05). Paw thermal withdrawal latency (PTWL) results of left and right feet in five groups had no significant difference before surgery (P > 0.05); after the establishment of neuropathic model, PTWL results in five groups were significantly decreased; however, PTWL results of left and right feet at 3 days after surgery in IT group were significantly higher than the two other pretreatment groups (P < 0.05); PTWL results of left and right feet at 7 and 14 days after surgery had no significant difference. Parecoxib sodium pretreatment can effectively improve the behaviors caused by neuropathic pain, and intrathecal injection is the most effective route of administration.

Cell Biochemistry and Biophysics 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, Related Products of isoxazole.

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

Liu, Meina published the artcileSimultaneous determination of parecoxib sodium and its active metabolite valdecoxib in rat plasma by UPLC-MS/MS and its application to a pharmacokinetic study after intravenous and intramuscular administration, Recommanded Product: Sodium ((4-(5-methyl-3-phenylisoxazol-4-yl)phenyl)sulfonyl)(propionyl)amide, the publication is Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences (2016), 220-229, database is CAplus and MEDLINE.

In this study, the authors developed and validated a new, rapid, specific and sensitive ultra-performance liquid chromatog.-tandem mass spectrometric (UPLC-MS/MS) method to simultaneously determine parecoxib sodium (PX) and its active metabolite, valdecoxib (VX), in rat plasma. Plasma samples were prepared by plasma protein precipitation combined with a liquid-liquid extraction method. The separation was carried out on a Kinetex C₁₈ column (2.1 mm × 50 mm, 2.6 μm) with a gradient elution using methanol (A) and a 2 mM ammonium acetate aqueous solution (B). The anal. was performed in less than 3 min with a flow rate of 0.2 mL/min. Ketoprofen was used as an internal standard (IS). Mass spectrometric detection was conducted with a triple quadrupole detector equipped with electrospray ionization in the neg. ion mode (ESI^–) using multiple reaction monitoring (MRM). The calibration curves were linear over the concentration ranges of 5-4000 ng/mL for PX and 5-2000 ng/mL for VX with all correlation coefficients greater than 0.998. The intra- and inter-day relative standard deviations (RSD) for both analytes were within 15% and the accuracy was within 85-115% at all quality control levels. The mean extraction recoveries for all analytes obtained from three concentrations of QC plasma samples were more than 89.0% efficient. Selectivity, matrix effect, dilution integrity and stability were also validated. The method was successfully used to investigate the pharmacokinetics of PX and VX in rat plasma after i.v. and i.m. administration of PX.

Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences 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

Yu, Qiuyang published the artcileValidated Stability-indicating RP-HPLC Method for the Determination of Parecoxib Sodium and Degradation Impurities in Bulk Drug, Related Products of isoxazole, the publication is Current Pharmaceutical Analysis (2017), 13(3), 271-278, database is CAplus.

Background: Parecoxib sodium (PCX), the selective cyclooxygenase (COX)-2 inhibitor, has aroused great interests among researchers mainly because of its central role in analgesic and antiinflammatory effects in a wide range of perioperative or postoperative procedures. The aim of the current study was to develop and validate a precise, accurate, and specific HPLC method systematically which could accomplish the stability indicating of PCX bulk drug and qualitation and quantization for the formed main impurity under the stressed conditions. Objective: Accomplishing the stability indicating of PCX bulk drug and qualitation and quantization for the formed main impurity under the stressed conditions. Methods: The study performed forced degradation testing on drug substances under varied conditions including alkali, acid, oxidation, photolysis, thermal and humidity using established stability-indicating high performance liquid chromatog. with photodiode array detector (HPLC-DAD). Results: The content of home-made bulk drug was 98.94% with RSD of 0.96% using our newly established method with respect to linearity, precision, specificity and accuracy. And we accomplished the stability indicating of PCX bulk drug and identified the newly formed main impurities including Impurity E (PCX), Impurity M, Impurity N, Impurity O, Impurity Q, and Impurity R under various stressed conditions. Conclusion: The stability-indicating HPLC method exhibited excellent performance, and the method was recommended for PCX bulk drug quality control anal. in the laboratory and pharmaceutical industry.

Current Pharmaceutical Analysis 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 C20H21ClN4O4, Related Products of isoxazole.

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

Liu, Guo-yan published the artcileEffect of parecoxib sodium combination of laryngeal mask airway on reaction of emergence agitation undergoing laparoscopic cholecystectomy, Computed Properties of 198470-85-8, the publication is Zhongguo Zhongxiyi Jiehe Waike Zazhi (2014), 20(2), 146-148, database is CAplus.

The effect of parecoxib sodium combination of the laryngeal mask airway on the reaction of emergence agitation undergoing laparoscopic cholecystectomy was observed Forty-five patients were randomly divided into group I (endotracheal extubation), group II (the laryngeal mask airway) and group III (parecoxib sodium combination of the laryngeal mask airway). Group I and II were given i.v. injection of normal saline 10mL and group III was given i.v. injection of parecoxib sodium 40 mg, 15 min before surgery. Sedation score was obviously higher in group II and group III than in group I (P<0.05); Agitation score was obviously lower in group II and group III than in group I (P<0.05); vital signs in group II and group III were stable than in group I before anesthesia, endotracheal extubation and after extubation (P<0.05) and vital signs were more stable in group III (P<0.05). Parecoxib sodium combination of the laryngeal mask airway can effectively and safely prevent emergence agitation undergoing laparoscopic cholecystectomy.

Zhongguo Zhongxiyi Jiehe Waike 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 C19H17N2NaO4S, Computed Properties of 198470-85-8.

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

Nogi, Keisuke published the artcileAromatic metamorphosis: conversion of an aromatic skeleton into a different ring system, Product Details of C18H12FN, the publication is Chemical Communications (Cambridge, United Kingdom) (2017), 53(29), 4055-4065, database is CAplus and MEDLINE.

Recent advances in the area of “aromatic metamorphosis”, where various aromatic compounds, such as dibenzothiophenes, dibenzofurans, and benzofurans, are transformed into a variety of ring systems using a multi-step strategy or ideally in one step has been reviewed.

Chemical Communications (Cambridge, United Kingdom) published new progress about 57103-14-7. 57103-14-7 belongs to isoxazole, auxiliary class Fused Tricycles,Carbazoles, name is 9-(4-Fluorophenyl)-9H-carbazole, and the molecular formula is C18H12FN, Product Details of C18H12FN.

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

Nakayama, Yuji published the artcileAn Efficient Synthesis of N-(Hetero)arylcarbazoles: Palladium-Catalyzed Coupling Reaction between (Hetero)aryl Chlorides and N-Carbazolylmagnesium Chloride, Quality Control of 57103-14-7, the publication is Advanced Synthesis & Catalysis (2015), 357(10), 2322-2330, database is CAplus.

An efficient method for the synthesis of N-(hetero)arylcarbazoles, useful compounds for functional materials, was reported. Various (hetero)aryl chlorides reacted with N-carbazolylmagnesium chloride in the presence of a palladium catalyst (0.05 to 0.2 mol%) prepared from allylpalladium(II) chloride dimer {[PdCl(allyl)]₂} and di-tert-butyl(2,2-diphenyl-1-methylcyclopropan-1-yl)phosphine (cBRIDP) under mild conditions (110°) in a short period of time (15 min. to 2 h) to give N-(hetero)arylcarbazoles in high yields. The reactions of bromochlorobenzenes proceeded in favor of the bromo group to afford N-(chlorophenyl)carbazoles in a highly selective manner. Functional materials for use in organic light-emitting diodes, such as 1,3-bis(9H-carbazol-9-yl)benzene, 2,6-bis(9H-carbazol-9-yl)pyridine, 4,4′-bis(9H-carbazol-9-yl)biphenyl and 1,3,5-tris(9H-carbazol-9-yl)benzene, were also obtained in high yields within 15 min. by the reaction of (hetero)aryl polyhalides. Optimization of the reaction conditions and a postulated catalytic cycle for the reaction were also discussed.

Advanced Synthesis & Catalysis published new progress about 57103-14-7. 57103-14-7 belongs to isoxazole, auxiliary class Fused Tricycles,Carbazoles, name is 9-(4-Fluorophenyl)-9H-carbazole, and the molecular formula is C18H12FN, Quality Control of 57103-14-7.

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

Huang, Xuelian published the artcileAnalysis of effect of levobupivacaine combined with tramadol on infiltration anesthetic analgesia of incision after lumbar intervertebral disc surgery, SDS of cas: 198470-85-8, the publication is Fujian Yiyao Zazhi (2015), 37(4), 111-113, database is CAplus.

Objective: To analyze effect of evobupivacaine combined with tramadol on infiltration anesthetic analgesia of incision after lumbar intervertebral disk surgery. Methods: 60 patients who were going to being subjected to lumbar intervertebral disk surgery were randomly divided into 3 groups, evobupivacaine plug tramadol group (A group), evobupivacaine group (B group) and evobupivacaine plug physiol. saline group (C group). The patients in the three groups were given corresponding anesthetic analgesia treatment, resp. If VAS scores of the patients were higher than 3, the patients were given pethidine, and VAS scores and dosages of pethidine used 0 (T₀), 2 (T₂), 4 (T₄), 8 (T₈), 12 (T₁₂) and 24 (T₂₄) h after the surgery were recorded. If VAS cores were greater than 5, the patients were given parecoxib sodium, and the time when parecoxib sodium was used and dosage of parecoxib sodium were recorded. Results: Within 24 h after the surgery, there were 3, 7 and 10 cases of nausea in the groups A, B and C, resp., there were 1, 4, and 4 cases vomiting in the groups A, B and C, resp., and no skin pruritus complication occurred in the three groups. No patient in the A group used parecoxib sodium, 3 patients in the B groups used parecoxib sodium 2 h after the surgery, and all patients in the C group were given parecoxib sodium within 1 h after the surgery. No patient in the A group used PCA, the time when the B group used PAC was (147.0 ± 167.3) min after the surgery, that in the C group was (13.6 ± 8.7) min after the surgery, and the difference was statistically significant (P < 0.05). No patient in the A group used pethidine, total dosage of pethidine used in the B group was (138.0 ± 76.2) mg, total dosage of pethidine used in the B group was (183.2 ± 86.3) mg, and the difference was statistically significant (P < 0.05). Compared with the group C, VAS core at the time point of T₀ in the groups A and B were statistically significant (P < 0.05). At the time points of T₂, T₄, T₈ and T₁₂, VAS scores of the group A were statistically significantly different from those of the group C. Conclusion: For the patients underwent lumbar intervertebral disk excision, levobupivacaine combined with tramadol for infiltration anesthesia of incision has better postoperative analgesia effect, causes lower VAS cores, and reduces use of opioid drugs. Combination of the two drugs is safe and effective, and is worthy of wide application.

Fujian Yiyao 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 C19H17N2NaO4S, SDS of cas: 198470-85-8.

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

Zhu, Yang-Zi published the artcileParecoxib prevents early postoperative cognitive dysfunction in elderly patients undergoing total knee arthroplasty: A double-blind, randomized clinical consort study, Product Details of C19H17N2NaO4S, the publication is Medicine (Philadelphia, PA, United States) (2016), 95(28), e4082, database is CAplus and MEDLINE.

Background: Trial design neuroinflammation and postoperative pain after surgery are increasingly reported in association with postoperative cognitive dysfunction (POCD). Parecoxib, a selective cyclooxygenase (COX)-2 inhibitor, is used for postoperative analgesia for its potent anti-inflammatory and analgesic effects. This study aimed to evaluate parecoxib’s effects on POCD in elderly patients undergoing total knee arthroplasty. Methods: Around 134 elderly patients undergoing total knee arthroplasty were randomly divided into parecoxib (group P) and control (groupC) groups, and treated with parecoxib sodium and saline, resp., shortly after induction of general anesthesia and 12-h postsurgery, resp. Perioperative plasma IL-1β, IL-6, TNF-α, and C-reactive protein (CRP) levels were measured. Postoperative pain was assessed following surgery. Neuropsychol. tests were performed before surgery, and 1 wk and 3 mo postoperation. Results: POCD incidence in group P was significantly lower compared with that of group C at 1 wk after surgery (16.7% vs 33.9%; P<0.05); no significant difference was found between groups C and P at 3-mo follow-up (9.7% vs 6.7%). Compared with group C values, visual analog pain scale (VAS) scores at 3, 6, and 12h after surgery were significantly lower in group P(P<0.05). Plasma IL-1β, IL-6, and TNF-α levels were lower in group P than in group C after the operation (P<0.05). No significant difference in the plasma CRP level was found between groups P and C. Conclusions: Parecoxib sodium decreases POCD incidence after total knee arthroplasty in elderly patients and may explain how this drug suppresses inflammation and acute postoperative pain caused by surgical trauma.

Medicine (Philadelphia, PA, United States) 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 C38H74Cl2N2O4, Product Details of C19H17N2NaO4S.

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

Fu, Weihua published the artcileEfficacy and Safety of Parecoxib/Phloroglucinol Combination Therapy Versus Parecoxib Monotherapy for Acute Renal Colic: A Randomized, Double-Blind Clinical Trial, Recommanded Product: Sodium ((4-(5-methyl-3-phenylisoxazol-4-yl)phenyl)sulfonyl)(propionyl)amide, the publication is Cell Biochemistry and Biophysics (2014), 69(1), 157-161, database is CAplus and MEDLINE.

To investigate whether the addition of phloroglucinol to parecoxib could improve the efficacy in patients with acute renal colic. Patients of acute renal colic were randomly allocated to receive i.v. Parecoxib 40 mg plus placebo or Parecoxib 40 mg plus phloroglucinol 80 mg, resp. Pain intensity was recorded using a visual analog scale (VAS) before drug administration and 5, 15, 30, 60, and 120 min after treatment start. The primary outcome was the mean pain intensity difference (PID) at each checkpoint and the effectiveness of drugs (≥50 ^decrease in VAS score at the end checkpoint). The need for rescue analgesics and the incidence of adverse effects were considered as secondary outcome of the study. Among 236 patients enrolled in the study, 119 patients received i.v. parecoxib plus placebo and 114 patients received i.v. parecoxib plus phloroglucinol, the remaining 3 patients given up treatment. Baseline demographics were similar between two groups. There are significant differences in the PID at 15 and 30 min between two groups (P_15 min = 0.011, P_30 min = 0.013). Rescue analgesics were required by 17 patients (14.3 )̂ receiving parecoxib, 7 patients (6.1 )̂ receiving parecoxib plus phloroglucinol (P = 0.041). There were no differences in PID at other checkpoints between two groups, as well as in the incidence of adverse events and the drug effectiveness. Parecoxib in combination with phloroglucinol for acute renal colic has a faster action, also reduces the demand of rescue analgesics.

Cell Biochemistry and Biophysics 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