Category: 169590-42-5

Wang, Shengju published the artcileA comparative study on the traditional versus modern yellow rice wine processing methods using Taohong Siwu Decoction for pharmaceutical production, HPLC of Formula: 169590-42-5, the publication is Journal of Ethnopharmacology (2022), 115114, database is CAplus and MEDLINE.

Taohong Siwu Decoction (THSWD) is based on the “First Recipe of Gynecol”. It is widely used in various blood stasis and deficiency syndromes, mainly in gynecol. blood stasis, irregular menstruation, and dysmenorrhea. THSWD has great demand in traditional Chinese medicine (TCM), gynecol., orthopedics, and internal medicine. According to classical records, three medicinal materials, namely Rehmanniae radix, Angelica sinensis, and Carthamus tinctorius, used in THSWD need to be “washed with yellow rice wine”. In the study of TCM prescriptions, the processing methods of medicinal materials not only needed to follow traditional records but also should consider modern tech. conditions. Many medicinal materials in the repertoire of classical prescriptions involve yellow rice wine processing. Determining the processing method for medicinal materials is a key and difficult problem in the research and development of classical prescriptions. With THSWD as the representative, this study analyzed differences between no processing method, the modern processing method of “stir-frying the materials with yellow rice wine,” and the traditional processing method of “washing with yellow rice wine”. We focused on three aspects: composition, efficacy, and endogenous metabolism This study aimed to provide a reference for research on the processing methods of medicinal materials used in classical prescriptions. UPLC-Q-Orbitrap HRMS was used to quickly identify and classify the main chem. compounds of THSWD. A model of primary dysmenorrhea (PD) was established using estradiol benzoate combined with oxytocin. The latent period and writhing time; the levels of serum PGF2α, PGE2, ET-1, and β-EP; and the pathol. sections of the uterus were observed to determine their pharmacodynamic differences. GC-TOF/MS was used to analyze the differences in serum metabolites in rats. A total of 54 active compounds were identified, and the results showed that catalpol and rehmapicroside disappeared following yellow rice wine processing. Compared with materials processed by the traditional method, the relative contents of 15 components, such as 5-hydroxymethylfurfural and digitalis C, increased in materials processed by the modern method. However, the relative contents of 16 components, such as hydroxysafflor yellow A, verbascoside, and ferulic acid, decreased in the modern processing method. The modern and classic processing methods acted on PD through different metabolic pathways. THSWD obtained by classical processing methods mainly treated PD through anti-inflammatory and estrogen metabolism pathways, whereas THSWD obtained by modern processing methods mainly treated PD through anti-inflammatory metabolic pathways. The study revealed the differences in different yellow rice wine processing methods in terms of chem. composition of the THSWD obtained, as well as the mechanisms of action for the treatment of PD. This study provides a reference for the clin. application of THSWD and development of classical prescription preparations

Journal of Ethnopharmacology 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 C6H10O3, HPLC of Formula: 169590-42-5.

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

Pearson, Caroline A. published the artcileWhen the BBB goes MIA, Application In Synthesis of 169590-42-5, the publication is Proceedings of the National Academy of Sciences of the United States of America (2022), 119(19), e2204159119, database is CAplus and MEDLINE.

A review. Epidemiol. studies implicate maternal immune activation (MIA) as a risk factor for a variety of neurodevelopmental disorders. Early MIA results in BBB disruption and inflammatory responses that lead to persistent postnatal structural and cellular defects associated with MIA, rescuable by celecoxib treatment. The findings advance our understanding of the developmental origins of MIA-associated cognitive deflicits and unveil a potential therapeutic intervention for the BBB dysfunction and chronic inflammation associated with neurodevelopmental disease. In addition, the data raise the possibility that the BBB alterations induced by MIA may also contribute to other diseases associated with chronic neuroinflammation. In this regard, MIA in the setting of the SARS-CoV-2 pandemic should alert health-care providers to this potential risk, warranting careful monitoring of the offspring in infected mothers.

Proceedings of the National Academy of Sciences of the United States of America 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, Application In Synthesis of 169590-42-5.

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

Neogi, Tuhina published the artcileObserved efficacy and clinically important improvements in participants with osteoarthritis treated with subcutaneous tanezumab: results from a 56-week randomized NSAID-controlled study, Name: 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, the publication is Arthritis Research & Therapy (2022), 24(1), 78, database is CAplus and MEDLINE.

A recent phase 3 study demonstrated that treatment with tanezumab, a nerve growth factor inhibitor, or nonsteroidal anti-inflammatory drugs (NSAIDs) improves pain and phys. function in participants with moderate-to-severe osteoarthritis (OA) of the hip or knee. Here, we evaluated the time course and clin. importance of these initial efficacy findings using a mixture of primary, secondary, and post hoc endpoints. Participants on stable NSAID therapy and with a history of inadequate response to other standard OA analgesics were enrolled in an 80-wk (56-wk treatment/24-wk safety follow-up), randomized, NSAID-controlled, phase 3 study primarily designed to assess the safety of tanezumab for moderate-to-severe OA of the knee or hip. Participants received oral NSAID (twice daily naproxen, celecoxib, or diclofenac) or s.c. tanezumab (2.5mg or 5mg every 8 wk). Non-responders were discontinued at week 16. Changes from baseline in WOMAC Pain and Phys. Function, Patients Global Assessment of Osteoarthritis (PGA-OA), and average pain in the index joint were compared between tanezumab and NSAID groups over the 56-wk treatment period. Clin. meaningful response (e.g., ≥30% and ≥50% improvement in WOMAC Pain and Phys. Function), rescue medication use, and safety were also assessed. All groups improved WOMAC Pain, WOMAC Phys. Function, PGA-OA, and average pain in the index joint over the 56-wk treatment period relative to baseline. Across all groups, improvements generally occurred from the time of first assessment (week 1 or 2) to week 16 and then slightly decreased from week 16 to 24 before stabilizing from weeks 24 to 56. The magnitude of improvement and the proportion of participants achieving ≥30% and ≥50% improvement in these measures was greater (unadjusted p≤0.05) with tanezumab than with NSAID at some timepoints on or before week 16. Adverse events of abnormal peripheral sensation, prespecified joint safety events, and total joint replacement surgery occurred more frequently with tanezumab than with NSAID. Tanezumab and NSAID both provided early and sustained (up to 56 wk) efficacy relative to baseline. Improvements in pain and function were clin. meaningful in a substantial proportion of participants. Adverse events of abnormal peripheral sensation and joint safety events occurred more frequently with tanezumab than with NSAID. Trial registration: ClinicalTrials.govNCT02528188. Registered on 19 July 2015.

Arthritis Research & Therapy 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, Name: 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide.

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

Lin, Jialiang published the artcilePoly(lactic acid-co-glycolic acid)-based celecoxib extended-release microspheres for the local treatment of traumatic heterotopic ossification, SDS of cas: 169590-42-5, the publication is Journal of Biomaterials Applications (2022), 36(8), 1458-1468, database is CAplus and MEDLINE.

Traumatic heterotopic ossification (THO) is a serious and common clin. post-traumatic complication for which there is no effective and safe drug treatment. Routine administration of nonsteroidal anti-inflammatory drugs (NSAIDs) after injury is extensively used approach for THO. However, serious adverse events can occur in the event of an overdose of NSAIDs. In our study, we have developed a poly(lactic acid-co-glycolic acid) (PLGA) microsphere by emulsifying solvent volatilization for the prolonged slow delivery of celecoxib (CLX). Three groups of celecoxib-poly(lactic acid-co-glycolic acid) microspheres (CLX-PLGA MPs) were prepared with particle sizes of 3.75±1.28μm, 49.56±17.15μm, and 94.98±42.53μm. Meanwhile, related parameters of microspheres in each group were studied: drug loading (DL), encapsulation rate (EE), and slow-release behavior. The DL and EE of the 3 CLX-PLGA MPs did not vary significantly, and subsequently, we selected the second drug loading microspheres with a retardation period of about 70 days for subsequent experiments Moreover, cellular and animal experiments suggest that the microspheres are biocompatible and can be safely applied to localized trauma tissue. Finally, it is demonstrated that CLX-PLGA MPs have an effect on inhibiting the osteogenic differentiation of bone marrow mesenchymal stem cells and have the potential to inhibit ectopic bone formation of the THO model in Sprague-Dawley rat. Therefore, this study suggests that CLX-PLGA MPs are expected to be applied topically in the early post-traumatic period to prevent the development of THO.

Journal of Biomaterials Applications 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

Herron, Alastair N. published the artcileδ-C-H Halogenation Reactions Enabled by a Nitrogen-Centered Radical Precursor, COA of Formula: C17H14F3N3O2S, the publication is Organic Letters (2022), 24(20), 3652-3656, database is CAplus and MEDLINE.

Herein, new hydrazonyl carboxylic acids RN(S(O)₂R¹)N=C(Me)C(O)OH (R = octyl, 2-(adamantan-1-yl)ethyl, 4-methylpentyl, etc.; R¹ = 4-methylphenyl, 4-methoxyphenyl, 4-bromophenyl, 4-(trifluoromethyl)phenyl) precursor to nitrogen-centered radicals and its application toward remote C-H fluorination and chlorination reactions of sulfonyl-protected alkyl amines R¹S(O)₂NHR² (R² = 4-fluorooctyl, 2-(2-fluorocyclobutyl)ethyl, 4-fluoro-4-methylpentyl, etc.) via 1,5-HAT were disclosed.

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, COA of Formula: C17H14F3N3O2S.

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

Ansari, Shaquib Rahman published the artcileHyperthermia-Induced In Situ Drug Amorphization by Superparamagnetic Nanoparticles in Oral Dosage Forms, Category: amides-buliding-blocks, the publication is ACS Applied Materials & Interfaces (2022), 14(19), 21978-21988, database is CAplus and MEDLINE.

Superparamagnetic iron oxide nanoparticles (SPIONs) generate heat upon exposure to an alternating magnetic field (AMF), which has been studied for hyperthermia treatment and triggered drug release. This study introduces a novel application of magnetic hyperthermia to induce amorphization of a poorly aqueous soluble drug, celecoxib, in situ in tablets for oral administration. Poor aqueous solubility of many drug candidates is a major hurdle in oral drug development. A novel approach to overcome this challenge is in situ amorphization of crystalline drugs. This method facilitates amorphization by mol. dispersion of the drug in a polymeric network inside a tablet, circumventing the phys. instability encountered during the manufacturing and storage of conventional amorphous solid dispersions. However, the current shortcomings of this approach include low drug loading, toxicity of excipients, and drug degradation Here, doped SPIONs produced by flame spray pyrolysis are compacted with polyvinylpyrrolidone and celecoxib and exposed to an AMF in solid state. A design of experiments approach was used to investigate the effects of SPION composition (Zn_0.5Fe_2.5O₄ and Mn_0.5Fe_2.5O₄), doped SPION content (10-20 wt %), drug load (30-50 wt %), and duration of AMF (3-15 min) on the degree of drug amorphization. The degree of amorphization is strongly linked to the maximum tablet temperature achieved during the AMF exposure (r = 0.96), which depends on the SPION composition and content in the tablets. Complete amorphization is achieved with 20 wt % Mn_0.5Fe_2.5O₄ and 30 wt % celecoxib in the tablets that reached the maximum temperature of 165.2 °C after 15 min of AMF exposure. Furthermore, manganese ferrite exhibits no toxicity in human intestinal Caco-2 cell lines. The resulting maximum solubility of in situ amorphized celecoxib is 5 times higher than that of crystalline celecoxib in biorelevant intestinal fluid. This demonstrates the promising capability of SPIONs as enabling excipients to magnetically induce amorphization in situ in oral dosage forms.

ACS Applied Materials & Interfaces 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, Category: amides-buliding-blocks.

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

Wang, Wei published the artcileScaffold Hopping Strategy to Identify Prostanoid EP4 Receptor Antagonists for Cancer Immunotherapy, Recommanded Product: 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, the publication is Journal of Medicinal Chemistry (2022), 65(11), 7896-7917, database is CAplus and MEDLINE.

Cancer cells can effectively suppress the natural immune response in humans, and prostaglandin E₂ (PGE₂) is a key mediator in the development of tumor cell resistance to immunotherapy. As a major contributor to PGE₂-elicited immunosuppressive activity, the EP4 receptor promotes tumor development and progression in the tumor microenvironment, and the development of selective and potent EP4 receptor antagonists should have promising potential for tumor immunotherapy. Aiming at improving the drug-like properties, a series of 4,7-dihydro-5H-thieno[2,3-c]pyran derivatives were designed and synthesized through a scaffold hopping strategy. The most promising compound 47 exhibited good EP4 antagonistic activity and excellent subtype selectivity, as well as favorable drug-like properties. It effectively suppressed the expression of multiple immunosuppression-related genes in macrophages. Meanwhile, oral administration of compound 47, alone or in combination with anti-PD-1 antibody, significantly enhanced the antitumor immune response and inhibited tumor growth in the mouse CT26 colon carcinoma model.

Journal of Medicinal Chemistry 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 C7H8BClO3, 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

Nikolos, Fotis published the artcileCell death-induced immunogenicity enhances chemoimmunotherapeutic response by converting immune-excluded into T-cell inflamed bladder tumors, Quality Control of 169590-42-5, the publication is Nature Communications (2022), 13(1), 1487, database is CAplus and MEDLINE.

Chemoimmunotherapy has recently failed to demonstrate significant clin. benefit in advanced bladder cancer patients; and the mechanism(s) underlying such suboptimal response remain elusive. To date, most studies have focused on tumor-intrinsic properties that render them “immune-excluded”. Here, we explore an alternative, drug-induced mechanism that impedes therapeutic response via disrupting the onset of immunogenic cell death. Using two immune-excluded syngeneic mouse models of muscle-invasive bladder cancer (MIBC), we show that platinum-based chemotherapy diminishes CD8+ T cell tumor infiltration and constraines their antitumoral activity, despite expression of activation markers IFNγ and granzyme B. Mechanistically, chemotherapy induces the release of prostaglandin E2 (PGE2) from dying cancer cells, which is an inhibitory damage-associated mol. pattern (iDAMP) that hinderes dendritic cell maturation. Upon pharmaceutical blockade of PGE2 release, CD8+ T cells become tumoricidal and display an intraepithelial-infiltrating (or inflamed) pattern. This “iDAMP blockade” approach synergizes with chemotherapy and sensitizes bladder tumors towards anti-PD1 immune checkpoint inhibitor therapy. These findings provide a compelling rationale to evaluate this drug combination in future clin. trials.

Nature Communications 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, Quality Control of 169590-42-5.

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

Matsunuma, Satoru published the artcileHigh concentration of oxaliplatin may be a risk factor for vascular pain, SDS of cas: 169590-42-5, the publication is Journal of Clinical Pharmacy and Therapeutics (2022), 47(4), 462-468, database is CAplus and MEDLINE.

Oxaliplatin (L-OHP) is an antineoplastic agent that frequently causes vascular pain. However, the risk factors for vascular pain are unclear, and prevention methods have not been established. We retrospectively investigated patients who were treated with L-OHP to examine the influence of patient characteristics and concomitant analgesic use on the incidence of vascular pain. We collected information about the presence or absence of vascular pain, age, sex, treatment dose and analgesic use of patients who received L-OHP at Tokyo Medical University Hachioji Medical Center. We analyzed the relevance of each factor between the vascular pain onset and non-onset groups. Thirty-two patients (average age: 68.6 years; 69.8% and 30.2% men and women, resp.) were classified into the vascular pain onset (n = 64) and non-onset groups (n = 68). The multivariate logistic regression anal. revealed that L-OHP concentration (>358.5 mg/L) was an independent determinant of vascular pain development (odds ratio: 2.422, 95% CI: 1.117-5.252). Intergroup differences in age, sex, body mass index, non-steroidal anti-inflammatory drug use, and underlying pain from cancer and other comorbidities were not significant. High L-OHP concentration was identified as a significant risk factor for L-OHP-induced vascular pain. Our results indicate that the dilution of L-OHP may reduce the incidence of vascular pain.

Journal of Clinical Pharmacy and Therapeutics 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

Gutierrez-Seijo, Alba published the artcileActivin A Sustains the Metastatic Phenotype of Tumor-Associated Macrophages and Is a Prognostic Marker in Human Cutaneous Melanoma, Category: amides-buliding-blocks, the publication is Journal of Investigative Dermatology (2022), 142(3_Part_A), 653-661.e2, database is CAplus and MEDLINE.

Tumor cells attract and dynamically interact with monocytes/macrophages to subvert their differentiation into tumor-associated macrophages (TAMs), which mainly promote immune suppression and neoplastic progression, but the pathways and microenvironmental cues governing their protumoral deviation are not completely understood. To identify the mol. pathways responsible for TAM differentiation, we screened the biomarkers secreted during melanoma-macrophage interactions using Quantibody microarrays and RNA sequencing of macrophages. We found that activin A, a member of the transforming GF family, plays an instrumental role in the cross-talk between melanoma cells and monocytes/macrophages, which results in the upregulation of distinct tumor-sustaining genes and the achievement of proinvasive and immunosuppressive functions of TAMs. Blockade of activin reduces the upregulation of part of these genes and prevents the acquisition of protumoral functions, facilitating human melanoma rejection by transferred human lymphocytes in a xenograft mouse model. Remarkably, screening of two independent cutaneous primary melanoma collections showed that activin A is enriched in TAMs and melanoma cells from patients with worse outcomes and constitutes a new and independent prognostic marker. Thus, we identify activin A as a key intermediary in the protumoral and immunosuppressive functions of TAMs, with significant potential as a disease biomarker as well as an immunotherapeutic target.

Journal of Investigative Dermatology 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, Category: amides-buliding-blocks.

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