Tag: M.W=350-400

Zu, Bing published the artcileCatalytic Enantioselective Construction of Chiroptical Boron-Stereogenic Compounds, Product Details of C24H22N2O2, the publication is Journal of the American Chemical Society (2021), 143(39), 16302-16310, database is CAplus and MEDLINE.

The construction of main group heteroatom-stereogenic compounds is of great importance due to their intriguing chem., phys., biol., and stereoelectronic properties. Despite that organoboron compounds are widely used in organic chem., the creation of a tetrahedral B-stereogenic center in one enantiomeric form remains highly challenging. Given the labile nature of ligands attached to the tetracoordinate B atom, only a handful of enantioenriched B-stereogenic compounds are reported via resolution or a chiral substrate-induced diastereoselective approach. To date catalytic asym. synthesis of B-stereogenic compounds has remained unknown. Here, the authors demonstrate the 1st catalytic enantioselective construction of B-stereogenic compounds via an asym. Cu-catalyzed azide-alkyne cycloaddition (CuAAC) reaction. This enantioselective CuAAC reaction not only gives access to a wide range of novel highly functionalized B-stereogenic heterocycles in high yields with good to excellent enantioselectivities but also produces optically active terminal alkyne and triazole moieties with various potential application prospects. Further transformation of the chiral tetracoordinate B compounds delivers several complex heterocyclic entities bearing B-stereogenic centers without the loss of enantiopurity. Also, the x-ray structure, the barrier to racemization, and the HOMO/LUMO gap of selected tetracoordinate B compounds were studied. Notably, these novel N,N π-conjugated B-stereogenic compounds exhibit bright fluorescence. The optical properties, including CD, quantum yield, and circular polarized luminescence spectroscopies, were examined These features expand the chem. space of the chiroptical B-based dye platform, which could have great potential applications in chiral optoelectronic materials.

Journal of the American Chemical Society 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 C7H10BNO3, Product Details of C24H22N2O2.

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

Zhang, Na published the artcileSynergistic analgesic effect of choline and parecoxib sodium in mice and its mechanism, Synthetic Route of 198470-85-8, the publication is Nanfang Yike Daxue Xuebao (2016), 36(11), 1536-1540, database is CAplus and MEDLINE.

Objectives: To investigate the synergistic analgesic effect of choline and parecoxib sodium and to study its mechanism. Methods: In male Kunming mice with acetic acid-induced writhing, ED₅₀ of choline and parecoxib sodium was administered via the tail vein at 2 h and 30 min before modeling, resp. and their combined use was determined In saline (control) group, ED₅₀ choline (C) group, ED₅₀ parecoxib sodium (P) group, and 1/2ED₅₀ choline and parecoxib sodium (1/2[C+P]) group, blood samples were collected from the eyeball 10 min after i.p. administration of acetic acid to detect the levels of IL-1, TNF-α, PGE₂, NF-κB, and I-κB levels using ELISA kits. Results: In the acetic acid-induced writhing model, the ED₅₀ of choline and parecoxib sodium was 8.64 and 6.33 mg/kg, and when combined, their ED₅₀ was 2.13 and 1.56 mg/kg, resp. The isobolograms of parecoxib sodium and choline showed that the measured ED₅₀ of the two drugs combined was below the theor. ED₅₀ value (P < 0.05) with a combination index (CI) of < 0.9. Compared with the control group, C group, P group, and 1/2 (C+P) group all showed significantly lowered IL-1 and TNF-α levels (P < 0.05), especially in 1/2 (C+P) group (P < 0.05). PGE₂ level was significantly lower in P group and 1/2 (C+P) group compared with the control group (P < 0.05). The level od NF-κB and I-κB was significantly lowered in C, P, and 1/2 (C+P) groups (P < 0.05), and the reduction was the most obvious in 1/2 (C+P) group (P < 0.05). Conclusions: Choline and parecoxib sodium has a synergistic analgesic effect, and their interactions may involve the in vivo expression of NF-κB.

Nanfang Yike Daxue Xuebao 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 C15H14BNO4S, Synthetic Route of 198470-85-8.

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

Qiu, Liang-cheng published the artcileEffects of preemptive parecoxib sodium versus flurbiprofen axetil on blood coagulation, Application of Sodium ((4-(5-methyl-3-phenylisoxazol-4-yl)phenyl)sulfonyl)(propionyl)amide, the publication is Linchuang Mazuixue Zazhi (2014), 30(11), 1087-1090, database is CAplus.

The effects of preemptive parecoxib sodium and flurbiprofen axetil on blood coagulation in patients undergoing radical mastectomy for breast cancer were compared. Ninety patients undergoing selective radical mastectomy were randomly allocated to three groups: 30 were injected with parecoxib sodium 40 mg (group P), 30 with flurbiprofen axetil 50 mg (group F) and 30 with normal saline (group N), each 10 mL during 10 min before induction of anesthesia. Total i.v. target-controlled infusion of remifentanil and propofol was used for anesthesia. Normal saline was the only liquid during operation. Three groups received patient controlled i.v. analgesia (PCIA) with sufentanil after surgery. Venous blood samples were taken from upper extremity before and at 30 min, 1 h, 3 h and 6 h after parecoxib, flurbiprofen axetil or normal saline administration for coagulation test, platelet count (Plt) and platelet aggregation rate (PAR), and the adverse reactions were recorded during 24 h after surgery. After 30 min of drugs administration, thrombin time (TT) of three groups was significantly extend (P<0.05); and fibrinogen (Fib) of groups F and N reduced significantly (P<0.05), which was significantly lower than that of group P (P<0.05). There were no significant differences between the other time points of coagulation parameters, Plt and PAR. The incidences of nausea arid vomiting within 24 h after surgery in groups P and F were reduced significantly compared with group N (P<0.05), the incidences of dizziness, sweating and itching had no differences, and there were no adverse reactions of gastrointestinal bleeding/ulcers and respiratory depression in all there groups. As to 50 mg of flurbiprofen axetil, preemptive parecoxib sodium 40 mg can temporarily enhance blood coagulation in patients undergoing radical mastectomy for breast cancer.

Linchuang Mazuixue 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, Application of Sodium ((4-(5-methyl-3-phenylisoxazol-4-yl)phenyl)sulfonyl)(propionyl)amide.

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

Cui, Xi-shun published the artcileDevelopment and Validation of the Production Process of Parecoxib Sodium Freeze-dried Preparation Based on Quality by Design, Application of Sodium ((4-(5-methyl-3-phenylisoxazol-4-yl)phenyl)sulfonyl)(propionyl)amide, the publication is Zhongguo Yaoxue Zazhi (Beijing, China) (2017), 52(15), 1337-1341, database is CAplus.

To prepare parecoxib sodium freeze-dried preparation, evaluate and validate the feasibility of the production process and quality reliability of the preparation Risk assessment of the production process of parecoxib sodium freeze-dried preparation was performed based on the method of quality by design (QbD). The key steps and key process parameters were identified. The critical quality attributes (CQAs)of the intermediates and final product were clarified, the validation protocol and acceptable standard were accordingly developed, and the production process was validated. The production process of parecoxib sodium freeze-dried preparation met the GMP requirements, and the intermediate and final products met the quality standards The established production process of pareeoxib sodium freeze-dried preparation is feasible and the product quality is controllable.

Zhongguo Yaoxue Zazhi (Beijing, China) 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, Application of Sodium ((4-(5-methyl-3-phenylisoxazol-4-yl)phenyl)sulfonyl)(propionyl)amide.

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

Chen, Jiang published the artcileInfluence of flurbiprofen and parecoxib sodium on behavior and spinal cord COX-2 expression in incision pain rats, Category: isoxazole, the publication is Zhongguo Yaowu Yu Linchuang (2014), 14(5), 600-601, database is CAplus.

Forty-eight SD rats were randomly divided into control group, 0.9% NaCl group, flurbiprofen group (0.9 mg/100 g) and parecoxib sodium group (0.6 mg/100 g). Behavior and pain score were observed COX-2 expression was determined by ELISA. Pain score and COX-2 expression of flurbiprofen group and parecoxib sodium group were significantly lower than those in NaCl group (P<0.05). And no significant difference of Pain score and COX-2 expression was found between flurbiprofen group and parecoxib sodium group (P>0.05). Flurbiprofen and parecoxib sodium both inhibits COX-2 expression in spinal cord and showed analgesic effect in incision pain rats.

Zhongguo 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, Category: isoxazole.

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

Zhou, Junyu published the artcileTherapeutic effect of parecoxib sodium on prevention of sore throat after laparoscopic cholecystectomy, Related Products of isoxazole, the publication is Jianyan Yixue Yu Linchuang (2021), 18(3), 368-371, database is CAplus.

Objective To observe the efficacy of parecoxib sodium in preventing postoperative sore throat after laparoscopic cholecystectomy. Methods A total of 130 patients with general anesthesia who underwent laparoscopic cholecystectomy from June 2018 to Jan. 2019 in Traditional Chinese Medicine Hospital of Beibei District were selected as research objects, and the patients were gender-specific, aged 21-67 years old, American society of anesthesiologists grade I, II, and were randomly divided into parecoxib sodium group (Group P) and saline group (Group S). Patients in group P received i.v. injection of parecoxib sodium 40 mg 10 min before the end of surgery, and patients in group S received an equal volum of normal saline. Visual analog scale/score (VAS) was recorded immediately after extubation, 2, 6, 12, and 24 h after surgery. The adverse reactions occurred during extubation were observed and recorded. The incidence of pharyngeal complications and the use of patient controlled i.v. analgesia (PCIA) at 6 h postoperatively, and QoR-15 (15-item quality of recovery scale) scores at 24, 48 h after surgery were recorded. Results VAS scores in the group P at the moment of extubation, 2, 6, and 12 h after surgery were lower than those in the group S, the number of PCIA compressions was less than that of the group S, the incidence of adverse reactions during extubation and complications in the throat at 6 h after surgery were significantly lower than those in group S, 15-item recovery quality scale scores at 24 and 48 h after surgery were significantly higher than that in group S, and the differences were statistically significant (P<0.05). Conclusion Parecoxib sodium can effectively reduce the incidence of sore throat after laparoscopic cholecystectomy.

Jianyan Yixue 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 C13H18N2, Related Products of isoxazole.

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

Deng, Fen published the artcileApplication effect of parecoxib sodium on postoperative analgesia in patients with craniotomy, SDS of cas: 198470-85-8, the publication is Liaoning Yixueyuan Xuebao (2016), 37(4), 61-64, database is CAplus.

Objective: To explore the application effect of parecoxib sodium on postoperative analgesia in patients with craniotomy. Methods: 90 cases of patients who underwent craniotomy in the neurosurgery department of our hospital from Feb. 2014 to Jan. 2015 were selected and randomly divided into the control group and the observation group, with 45 patients in each group. The patients in the observation group were treated with i.v. injection of parecoxib sodium, while the patients in the control group were given the equal amount of normal saline. The heart rate (HR), respiratory frequency (RR) and mean arterial pressure (MAP) in two groups were monitored by professional medical staff before the operation and 1, 6, 12, 24 h after the operation, and the VAS score, the restless score (RS score) and the sedation score (Ramsay score) in two groups were investigated 1, 6, 12 and 24 h after operation. The complications of all patients, 24 h after operation, were statistically analyzed. Results: The levels of HR and MAP in the two groups 1h and 6h after operation were significantly higher than those before operation, while the levels of HR and MAP in the observation group 1h and 6h after operation were significantly lower than those in the control group. The differences were statistically significant (P<0.05). The levels of HR and MAP in the two groups 12 h and 24 h after operation were not significantly different from those before operation (P>0.05). In addition, the level of RR in the two groups 1, 6, 12 and 24 h after operation was not significantly different from that before operation (P>0.05). The VAS and RS scores in the observation group were significantly lower than those in the control group 1, 6, 12 and 24 h after operation, whereas the Ramsay score was significantly higher than that in the control group. The differences were statistically significant (P<0.05). There were no significant differences in the VAS, RS and Ramsay scores in the two groups at each time point after operation (P>0.05). The incidence of complications in the observation group was significantly lower than that in the control group (χ²=1.984, P<0.05). Conclusion: Parecoxib sodium has analgesic and sedative effect on patients after craniotomy, which can improve the postoperative vital signs and reduce the incidence of complications of patients.

Liaoning Yixueyuan Xuebao 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

Qiu, Shuang published the artcileEffect of preemptive analgesia with parecoxib sodium combined with sufentanil postoperative analgesia on early cognitive function in elderly patients after operation, Application In Synthesis of 198470-85-8, the publication is Shiyong Yaowu Yu Linchuang (2016), 19(4), 425-429, database is CAplus.

To investigate the effect of preemptive analgesia with parecoxib sodium combined with sufentanil analgesia on postoperative cognitive function in elderly patients undergoing thoracic surgery. Sixty ASA I-II patients aged 65-75 years undergoing lung resection were randomly divided into two groups: parecoxib group (n = 30) and control group (n = 30). Parecoxib sodium (40 mg) + normal saline (5 mL) was injected i.v. after anesthesia induction in parecoxib group. Same volume saline was injected i.v. after anesthesia induction in control group. Patient-controlled i.v. analgesia with sufentanil 2 μg/kg and ramosetron hydrochloride 0.6 mg was used. At 2 h, 12 h and 24 h after operation, the pain score was evaluated by VAS score which should be less than 3. If VAS score was greater than 3, a bolus of PCIA was allowed until the analgesia was relieved. Cognitive function was assessed by Mini-Mental state examination (MMSE) at 1 d before operation and 2 h, 12 h and 24 h after operation. The total amount of sufentanil was recorded. Compared with control group, the incidence of postoperative cognitive dysfunction in parecoxib group was lower (P < 0.05), and the MMSE scores at 2 h, 12 h and 24 h after operation decreased more significantly (P < 0.05). The PCIA number of patients after compression in parecoxib group was less than that of control group with lower total amount of sufentanil and VAS score at 2 h, 12 h and 24 h after operation (P < 0.05). The incidence of adverse reaction (such as respiratory depression, nausea and vomiting) in parecoxib group was lower than that of control group (P < 0.05). Parecoxib sodium preemptive analgesia combined with sufentanil postoperative analgesia can effectively relieve the postoperative pain of elderly patients undergoing lung resection. Parecoxib sodium preemptive analgesia can reduce the risk of early period POCD and postoperative sufentanil consumption, and decrease the incidence of adverse reaction.

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, Application In Synthesis of 198470-85-8.

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

Zhang, Wei published the artcileEffect of parecoxib sodium on anesthesia effect by propofol combined with fentanyl and postoperative recovery in elderly patients with laparoscopic surgery, Recommanded Product: Sodium ((4-(5-methyl-3-phenylisoxazol-4-yl)phenyl)sulfonyl)(propionyl)amide, the publication is Hainan Yixueyuan Xuebao (2016), 22(12), 1279-1282, database is CAplus.

Objective: To study the effect of parecoxib sodium on anesthesia effect by propofol combined with fentanyl and postoperative recovery in elderly patients with laparoscopic surgery. Methods: A total of 80 elderly patients who received laparoscopic surgery in our hospital from May 2013 to Dec. 2015 were selected for study and randomly divided into observation group who received parecoxib sodium + propofol combined with fentanyl anesthesia and control group who received propofol combined with fentanyl anesthesia, and then pain threshold and serum indicators of two groups were compared. Results: 2h, 4h, 6h, 8h, 10 hand 12hafter surgery, pain threshold EI50 of observation group was significantly higher than that of control group; serum Glu, PS, histamine, 5-HT, MCP-1, CCR2, JAK2, STAT3, p38 MAPK, PX1, Orexin, IRAK1, TRAF6 and FcγRI contents of observation group were significantly lower than those of control group; serum GABA andβ-EP contents of observation group were significantly higher than those of control group. Conclusions: Parecoxib sodium has inhibiting effect on the pain perception of propofol combined with fentanyl anesthesia for elderly patients with laparoscopic surgery and can reduce the synthesis of pain neurotransmitters, inflammatory factors and related mols.

Hainan Yixueyuan Xuebao 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 C12H19BrS, Recommanded Product: Sodium ((4-(5-methyl-3-phenylisoxazol-4-yl)phenyl)sulfonyl)(propionyl)amide.

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

Camu, F. published the artcileParecoxib, propacetamol, and their combination for analgesia after total hip arthroplasty: a randomized non-inferiority trial, SDS of cas: 198470-85-8, the publication is Acta Anaesthesiologica Scandinavica (2017), 61(1), 99-110, database is CAplus and MEDLINE.

Background : This study assessed non-inferiority of parecoxib vs. combination parecoxib+propacetamol and compared the opioid-sparing effects of parecoxib, propacetamol, and parecoxib+propacetamol vs. placebo after total hip arthroplasty. Methods : In this randomized, placebo-controlled, parallel-group, non-inferiority study, patients received one of four IV treatments after surgery: parecoxib 40 mg bid (n = 72); propacetamol 2 g qid (n = 71); parecoxib 40 mg bid plus propacetamol 2 g qid (n = 72); or placebo (n = 38) with supplemental IV patient-controlled analgesia (morphine). Patients and investigators were blinded to treatment. Pain intensity at rest and with movement was assessed regularly, together with functional recovery (modified Brief Pain Inventory-Short Form) and opioid-related side effects (Opioid-Related Symptom Distress Scale) questionnaires up to 48 h. Results : After 24 h, cumulative morphine consumption was reduced by 59.8% (P < 0.001), 38.9% (P < 0.001), and 26.8% (P = 0.005) in the parecoxib+propacetamol, parecoxib, and propacetamol groups, resp., compared with placebo. Parecoxib did not meet criteria for non-inferiority to parecoxib+propacetamol. Parecoxib+propacetamol and parecoxib significantly reduced least-squares mean pain intensity scores at rest and with movement compared with propacetamol (P < 0.05). One day after surgery, parecoxib+propacetamol significantly reduced opioid-related symptom distress and decreased pain interference with function compared with propacetamol or placebo. Conclusion : Parecoxib and parecoxib+propacetamol provided significant opioid-sparing efficacy compared with placebo; non-inferiority of parecoxib to parecoxib+propacetamol was not demonstrated. Opioid-sparing efficacy was accompanied by significant reductions in pain intensity on movement, improved functional outcome, and less opioid-related symptom distress. Study medications were well tolerated.

Acta Anaesthesiologica Scandinavica 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