Category: 169590-42-5

Guo, Wei published the artcileImrecoxib versus celecoxib as postoperative analgesia for patients receiving arthroscopic knee surgery: a randomized, controlled, non-inferiority study, HPLC of Formula: 169590-42-5, the publication is Inflammopharmacology (2022), 30(3), 875-881, database is CAplus and MEDLINE.

Objective: Imrecoxib is a novel cyclooxygenase-2 inhibitor independently developed in China, which exhibits a good efficacy and tolerance in orthopedic disorders. The current study aimed to further compare its efficacy and safety with celecoxib as postoperative analgesia in arthroscopic knee surgery (AKS). Methods: Patients receiving AKS were enrolled and randomly assigned to imrecoxib (n = 64) and celecoxib (n = 62) group to receive analgesia for 72 h after surgery. Pain at rest and movement, pethidine consumption, patient′s satisfaction, Lysholm score, and adverse events were assessed after AKS. Meanwhile the upper limit of 95CI of pain-score mean difference (MD) between imrecoxib and celecoxib was calculated, then, the non-inferiority was defined if the all-time-point upper limits of 95CI less than 1. Results: Imrecoxib was non-inferior to celecoxib for alleviating pain at rest (upper limit of 95CI of MD ranging from 0.443 to 0.782, all time-point values less than 1); as well as for attenuating pain at movement (upper limit of 95CI of MD ranging from 0.398 to 0.582, all time-point values less than 1). Moreover, rescue analgesia rate (P = 0.583), pethidine consumption (P = 0.454), patient′s satisfaction at 72 h (P = 0.408), and Lysholm score at M3 (P = 0.776) were of no difference between imrecoxib group and celecoxib group. Addnl., the main adverse events in two groups were nausea (P = 0.425), constipation (P = 1.000), vomiting (P = 0.715), headache (P = 1.000), and dizziness (P = 0.667), which were mild and manageable. Conclusion: Imrecoxib is non-inferior to celecoxib in postoperative analgesia and exhibits an acceptable tolerance in patients undergoing AKS.

Inflammopharmacology published new progress about 169590-42-5. 169590-42-5 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Immunology/Inflammation,COX, name is 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C17H14F3N3O2S, HPLC of Formula: 169590-42-5.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Shi, Zhaojiang published the artcileElectrochemical Migratory Cyclization of N-Acylsulfonamides, HPLC of Formula: 169590-42-5, the publication is Angewandte Chemie, International Edition (2022), 61(30), e202206058, database is CAplus and MEDLINE.

Herein a facile electrochem. migratory cyclization of N-acylsulfonamides was reported to access a diverse array of benzoxathiazine dioxides I [R = H, 2-OMe, 4-F, etc.; R¹ = H, Ph, 2-pyridyl, etc.]. The inclusion of electrochem. was crucial for realizing such a novel transformation, which is substantiated both by the experiments and d.-functional-theory calculations

Angewandte Chemie, International Edition published new progress about 169590-42-5. 169590-42-5 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Immunology/Inflammation,COX, name is 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C7H16ClNO2, HPLC of Formula: 169590-42-5.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Wu, Ziying published the artcileAssociation between tramadol use and risk of pneumonia in the middle-aged and elderly populations: a propensity-score matched cohort study, SDS of cas: 169590-42-5, the publication is European Journal of Pain (Oxford, United Kingdom) (2022), 26(6), 1245-1255, database is CAplus and MEDLINE.

Tramadol is a widely used weak opioid; however, the evidence for its safety profile in respiratory system needs addnl. information. We aimed to examine whether tramadol use is associated with an increased risk of pneumonia in the general population. We conducted five propensity-score (PS) matched cohort studies in The Health Improvement Network database. Participants aged ≥50-years initiated tramadol were compared with those initiated one of the following analgesics: codeine (n = 144,506), naproxen (n = 113,028), diclofenac (n = 74,297), celecoxib (n = 42,538), or etoricoxib (n = 27,232). The outcome was incident pneumonia. During 6-mo follow-up, 395 pneumonia (5.6/1000 person-years) occurred in the tramadol group and 414 pneumonia (5.9/1000 person-years) occurred in the PS matched codeine group. Compared with codeine group, the risk of pneumonia was lower in the tramadol group (hazard ratio [HR] = 0.63, 95% confidence interval [CI]: 0.49-0.82) during the first 30-day follow-up, but comparable between groups over the entire 6-mo follow-up (HR = 0.95, 95%CI: 0.83-1.09). In addition, the risk of pneumonia was higher in the tramadol group than that in the PS matched naproxen (HR = 1.68, 95%CI: 1.37-2.06), diclofenac (HR = 1.63, 95%CI: 1.31-2.03), celecoxib (HR = 1.64, 95%CI: 1.20-2.24) or etoricoxib (HR = 1.61, 95%CI: 1.04-2.49) group. The present study indicated that tramadol initiators had a lower risk of incident pneumonia than codeine initiators during the short-time follow-up, but had a comparable pneumonia risk compared with codeine initiators and had a higher risk of pneumonia compared with NSAIDs initiators over the entire 6-mo follow-up duration. Confirmation of the present findings and determination of the underlying mechanism will require more studies. Tramadol might not be a safer alternative analgesic to codeine or NSAIDs. Both of health-care providers and patients may need to be on alert for its safety profile in respiratory system in future clin. practice.

European Journal of Pain (Oxford, United Kingdom) published new progress about 169590-42-5. 169590-42-5 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Immunology/Inflammation,COX, name is 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C4H11NO, SDS of cas: 169590-42-5.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Zhang, Tian-Yi published the artcileNew ursolic acid derivatives bearing 1,2,3-triazole moieties: design, synthesis and anti-inflammatory activity in vitro and in vivo, Formula: C17H14F3N3O2S, the publication is Molecular Diversity (2022), 26(2), 1129-1139, database is CAplus and MEDLINE.

In order to discover novel anti-inflammatory agents, three series of compounds obtained by appending 1,2,3-triazole moieties on ursolic acid I [n = 3; R¹ = H, 2-F, 4-Me, 3,4-(CH₃)₂], II [R² = H, 3-OMe, 2,4-(CH₃)₂, 3-CF₃, 2,4-Cl₂; X = O, NH], III (R³ = Ph, 2,3-dimethoxyphenyl, furan-2-yl, etc.) were designed and synthesized. All compounds have been screened for their anti-inflammatory activity by using an ear edema model. The potent anti-inflammatory compound was subjected to in vitro cyclooxygenase COX-1/COX-2 inhibition assays. In general, the derivatives were found to be potent anti-inflammatory activity. Especially, the compound I (n = 3; R³ = 2,3-dimethoxyphenyl) (IV) exhibited the strongest activity of all of the compounds prepared, with 82.81% inhibition after i.p. administration, which was better than celecoxib as a pos. control. Mol. docking results unclose the rationale for the interaction of the compound IV with COX-2 enzyme. Further studies revealed that compound IV exhibited effective COX-2 inhibitory activity, with half-maximal inhibitor concentration (IC₅₀) value of 1.16μM and selectivity index (SI = 64.66) value close to that of celecoxib (IC₅₀ = 0.93μM, SI = 65.47). Taken together, these results could suggest a promising chemotype for development of new COX-2-targeting anti-inflammatory agent.

Molecular Diversity published new progress about 169590-42-5. 169590-42-5 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Immunology/Inflammation,COX, name is 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C10H11NO4, Formula: C17H14F3N3O2S.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Rao, Chinthalapally V. published the artcileAnti-inflammatory Drugs Decrease the PD-L1 Expression and Increase the CD8⁺ T-Cell Infiltration, Synthetic Route of 169590-42-5, the publication is Cancer Prevention Research (2022), 15(4), 209-211, database is CAplus and MEDLINE.

In this issue of Cancer Prevention Research, Cecil and colleagues show that nonsteroidal anti-inflammatory drugs (NSAID), celecoxib and naproxen, decrease the expression of programmed death-ligand 1 (PD-L1) and increase the influx of Type I tumor-infiltrating lymphocytes in colonic tumors. Importantly, both decrease of PD-L1 expression and increase of CD8+ T cells were associated with the inhibition of COX-2/PGE2 pathway in vitro and syngeneic colonic tumor xenograft models. This study clearly suggests that NSAIDs regulate the intratumoral immunity multiple ways, including suppression of expression of immune checkpoint blockade. Thus, NSAIDs should be considered as chemopreventive for patients with PD-L1-pos. colonic polyp.

Cancer Prevention Research published new progress about 169590-42-5. 169590-42-5 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Immunology/Inflammation,COX, name is 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C17H14F3N3O2S, Synthetic Route of 169590-42-5.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Ball, Nicholas D. published the artcileSulfondiimidamides unlocked as new S(VI) hubs for synthesis and drug discovery, Recommanded Product: 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, the publication is Chem (2022), 8(4), 907-909, database is CAplus.

A review. Despite their promise as drug targets, access to nitrogen-rich S(VI) compounds has been a significant synthetic challenge. In this issue of Chem, Zhang and Willis explore a new class of S(VI) compounds-sulfondiimidamides-providing robust strategies toward their synthesis, derivation, and promise as new sulfonamide bioisosteres.

Chem published new progress about 169590-42-5. 169590-42-5 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Immunology/Inflammation,COX, name is 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C17H14F3N3O2S, Recommanded Product: 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Yang, Peiying published the artcileCelecoxib colorectal bioavailability and chemopreventive response in patients with familial adenomatous polyposis, Recommanded Product: 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, the publication is Cancer Prevention Research (2022), 15(4), 217-223, database is CAplus and MEDLINE.

Why celecoxib exerts chemopreventive activity in only some familial adenomatous polyposis (FAP) patients remains poorly understood. We conducted a phase II clin. study to identify potential predictive biomarkers for celecoxib chemopreventive activity in FAP. Twenty-seven patients with FAP completed a 6-mo oral course of 400 mg of celecoxib twice a day; they underwent colonoscopies before and after celecoxib treatment to assess colorectal polyp tumor burden and to obtain normal and polyp colorectal biopsies to measure celecoxib, 13-S-hydroxyoctadecadienoic acid (13-HODE), 15-HETE, 12-HETE, and LTB4 levels by LC/MS-MS. Celecoxib levels in sera from those patients were also measured before treatment and after 2, 4, and 6 mo of treatment. Nineteen of the 27 patients experienced a response to celecoxib, with a = 28% reduction of colonic polyp burden on the basis of a reproducible quant. assessment of colonoscopy results. Celecoxib levels were significantly lower in polyp tissues than in normal colorectal tissues. Celecoxib levels in sera and normal colorectal tissues were correlated in patients who experienced a response to celecoxib but not in those who did not. Among the measured lipoxygenase products, only 13-HODE levels were significantly lower in polyp tissues than in normal tissues. Our findings demonstrate the differential bioavailability of celecoxib between normal and polyp tissues and its potential effects on clin. response in patients with FAP.

Cancer Prevention Research published new progress about 169590-42-5. 169590-42-5 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Immunology/Inflammation,COX, name is 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C8H6F3NO, Recommanded Product: 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Zhao, Lulu published the artcileElectrochemical Synthesis of β-Functionalized Ketones via Ring-Opening of Cycloalkanols, SDS of cas: 169590-42-5, the publication is Organic Letters (2022), 24(24), 4421-4426, database is CAplus and MEDLINE.

The electrochem. deconstructive functionalization of cycloalkanols with nucleophiles was studied, which allowed functionalization to occur exclusively at the β-position of ketones. The substrate scope includes a wide range of cycloalkanols as well as diverse N, O, C and P-centered nucleophiles, providing ready access to β-functionalized ketones as products. Mechanistic studies support the generation of α,β-unsaturated ketones as key intermediates followed by Michael addition with nucleophiles.

Organic Letters published new progress about 169590-42-5. 169590-42-5 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Immunology/Inflammation,COX, name is 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C13H10F2, SDS of cas: 169590-42-5.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Du, Xian published the artcileHydrosulfonylation of Alkenes with Sulfonyl Imines via Ir/Cu Dual Photoredox Catalysis, SDS of cas: 169590-42-5, the publication is Organic Letters (2022), 24(22), 3944-3949, database is CAplus and MEDLINE.

Here utilizing sulfonyl imines as sulfonyl radical precursors for hydrosulfonylation of activated alkenes via visible-light irradiation was reported. By preinstallation of functional groups into the sulfonamides and subsequent hydrosulfonylation, a variety of complex sulfones were synthesized with good efficiency under Ir/Cu dual photoredox catalysis. Addnl., this protocol expands the research in late-stage N-S bond modification in sulfonamides.

Organic Letters published new progress about 169590-42-5. 169590-42-5 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Immunology/Inflammation,COX, name is 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C17H14F3N3O2S, SDS of cas: 169590-42-5.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Cai, Zhuochang published the artcileCelecoxib, Beyond Anti-inflammation, Alleviates Tendon-Derived Stem Cell Senescence in Degenerative Rotator Cuff Tendinopathy., Related Products of amides-buliding-blocks, the publication is The American journal of sports medicine (2022), 50(9), 2488-2496, database is MEDLINE.

BACKGROUND: Degenerative rotator cuff tendinopathy (RCT) is associated with the senescence of tendon-derived stem cells (TDSCs). Nonsteroidal anti-inflammatory drugs have been demonstrated to alleviate age-associated inflammation (inflamm-aging)-induced cellular senescence of skeletal stem/progenitor cells. However, whether they can alleviate degenerative RCT through reducing inflamm-aging-related TDSC senescence is still unknown. PURPOSE: To assess whether celecoxib can prevent the inflamm-aging-related cellular senescence of TDSCs. STUDY DESIGN: Controlled laboratory study. METHODS: TDSCs were isolated from degenerative RCT tendons (S-TDSCs) and healthy hamstring tendons (Y-TDSCs), and the cellular senescence of TDSCs was evaluated. Thereafter, the senescent TDSC-conditioned medium (SEN-CM) was collected to culture Y-TDSCs with or without celecoxib. The effects of celecoxib on TDSC senescence were examined by assaying the expression of aging-related markers. Furthermore, the level of the NF-κB pathway was determined by Western blot analysis to explore the underlying mechanism. Its effects on preventing dysfunction of inflamm-aging-induced senescent TDSCs were also determined using multilineage differentiation assay. RESULTS: S-TDSCs showed increased senescence-associated β-galactosidase activity and enhanced expression of γ-H2AX, p21^CIP1A, p16^INK4A, and senescence-associated secretory phenotype factors. SEN-CM accelerated the senescence progress of Y-TDSCs, resulting in an increase in senescence markers. To some extent, celecoxib treatment could prevent the detrimental effects of inflamm-aging on Y-TDSCs. The level of the NF-κB pathway was increased in the SEN-CM group but decreased with the use of celecoxib. Moreover, the reduced senescence of TDSCs resulted in preservation of the TDSC tenogenic potential. CONCLUSION: Celecoxib treatment can prevent inflamm-aging-induced TDSC senescence, which holds potential for alleviating the development of degenerative RCT. CLINICAL RELEVANCE: In addition to relieving the symptoms of patients with RCT, treatment with celecoxib, a common nonsteroidal anti-inflammatory drug, may defer the development of RCT and prevent rotator cuff tears by delaying TDSC senescence.

The American journal of sports medicine published new progress about 169590-42-5. 169590-42-5 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Immunology/Inflammation,COX, name is 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C17H14F3N3O2S, Related Products of amides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics