Month: December 2022

Hayat, Waseem published the artcileInsight into the degradation of methomyl in water by peroxymonosulfate, Application In Synthesis of 14294-10-1, the publication is Journal of Environmental Chemical Engineering (2021), 9(4), 105358, database is CAplus.

Methomyl (MET) is a carbamate pesticide frequently used in agriculture, globally. Its high solubility makes it a potential water pollutant. MET can be removed by peroxymonosulfate (PMS)-based advanced oxidation processes. This study explains MET degradation by PMS-Only, pyrite (PyR)-PMS and zero-valent iron (ZVI)-PMS systems. The degradation by PMS-Only, PyR-PMS and ZVI-PMS systems was 85.4%, 94.9% and 87.0%, resp. The generation of reactive oxygen species (ROS) and their role in degradation was elucidated by ESR (EPR) and free-radical quenching analyses, resp. EPR anal. indicated the presence of sulfate (SO•^–₄) and hydroxyl (•OH) radicals. The degradation in PMS-Only and ZVI-PMS systems was not significantly inhibited by tert-Bu alc. (TBA) and methanol (MeOH), which suggests that the degradation in both systems was not majorly carried out by SO•^–₄ and •OH. However, furfuryl acid (FFA) resulted in reduced degradation by applied systems, which showed that singlet oxygen (¹O₂) was mainly responsible for degradation in all systems. These results showed that MET was majorly degraded by non-radical PMS oxidation PMS-Only system resulted in an almost equal degradation, compared with PyR-PMS and ZVI-PMS systems. So, detailed anal. was carried out for PMS-Only system. Hence, experiments were conducted to investigate the effect of PMS concentration, MET concentration, pH and temperature on the degradation by PMS-Only system, which showed that PMS-Only system was efficient from pH 5.0 to pH 9.0, and from 10.0 °C to 40.0 °C. Further, PMS-Only system has a potential for effective degradation in real waters because it resulted in 66.5%, 63.7% and 60.4% degradation in tap water, lake water and sewage water, resp.

Journal of Environmental Chemical Engineering published new progress about 14294-10-1. 14294-10-1 belongs to amides-buliding-blocks, auxiliary class Morpholine,Thiourea,Amine,Amide, name is Morpholine-4-carbothioamide, and the molecular formula is C5H10N2OS, Application In Synthesis of 14294-10-1.

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

Ma, Xinyan published the artcileGenotoxicity of chloroacetamide herbicides and their metabolites in vitro and in vivo, Recommanded Product: 2-Chloroacetamide, the publication is International Journal of Molecular Medicine (2021), 47(6), 103, database is CAplus and MEDLINE.

The toxicity of chloroacetamide herbicide in embryo development remains unclear. Acetochlor (AC) is a chloroacetamide that metabolizes into 2-ethyl-6-methyl-2-chloroacetanilide (CMEPA) and 6-ethyl-o-toluidine (MEA). The present study determined the potential effect of AC and its metabolites on embryo development. Both HepG2 cells and zebrafish embryos were exposed to AC, CMEPA and MEA in the presence or absence of co treatment with anti reactive oxygen species (ROS) reagent N acetylcysteine. The generation of ROS, levels of superoxide dismutase (SOD) and glutathione (GSH) in HepG2 cells and lactate dehydrogenase (LDH) leakage from HepG2 cells were investigated. The effects of AC, CMEPA and MEA on DNA breakage, MAPK/ERK pathway activity, viability and apoptosis of HepG2 cells were examined by comet assay, western blotting, MTT assay and flow cytometry, resp. Levels of LDH, SOD and GSH in zebrafish embryos exposed to AC, CMEPA and MEA were measured. The hatching and survival rates of zebrafish embryos exposed to AC, CMEPA and MEA, were determined, and apoptosis of hatched fish was investigated using acridine orange staining. The present data showed AC, CMEPA and MEA induced generation of ROS and decreased levels of SOD and GSH in HepG2 cells, which in turn promoted DNA breakage and LDH leakage from cells, ultimately inhibiting cell viability and inducing apoptosis, as well as phosphorylation of JNK and P38. However, co treatment with N-acetylcysteine alleviated the pro apoptosis effect of AC and its metabolites. Moreover, exposure to AC, CMEPA and MEA lead to toxicity of zebrafish embryos with decreased SOD and GSH and increased LDH levels and cell apoptosis, ultimately decreasing the hatching and survival rates of zebrafish, all of which was attenuated by treatment with N-acetylcysteine. Therefore, AC and its metabolites (CMEPA and MEA) showed cytotoxicity and embryo development toxicity.

International Journal of Molecular Medicine published new progress about 79-07-2. 79-07-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Aliphatic hydrocarbon chain,Amide,Inhibitor, name is 2-Chloroacetamide, and the molecular formula is C2H4ClNO, Recommanded Product: 2-Chloroacetamide.

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

Jiang, Wenxiao published the artcileEffects of Different Nonsteroidal Anti-Inflammatory Drugs Combined with Platelet-Rich Plasma on Inflammatory Factor Levels in Patients with Osteoarthritis., Computed Properties of 169590-42-5, the publication is Journal of healthcare engineering (2022), 1979892, database is MEDLINE.

Objective: To investigate the effects of different nonsteroidal anti-inflammatory drugs combined with platelet-rich plasma on inflammatory factor levels in patients with osteoarthritis. Methods: The clinic data of 120 patients with osteoarthritis who were treated in our hospital (June 2019-June 2021) were retrospectively reviewed. All the patients were given platelet-rich plasma. According to the different nonsteroidal anti-inflammatory drugs the patients received, they were equalized into diclofenac sodium group, celecoxib group, and iguratimod group, with 40 cases in each group. After treatment, the patients’ clinical efficacy was compared and analyzed. Results: After treatment, the pain degrees of the patients in the three groups were gradually reduced. After 4 weeks and 8 weeks of treatment, the statistical differences in the scores of Visual Analogue Scale (VAS) were found among the three groups. Specifically, compared with the other two groups, the iguratimod group had remarkably lower VAS scores (P < 0.05) and the celecoxib group had signally lower VAS scores compared with the diclofenac sodium group (P < 0.05). After treatment, the inflammatory factor levels of interleukin-6 (IL-6), tumor necrosis factor-α (TNF-α), and high-sensitivity C-reactive protein (hs-CRP) in the diclofenac sodium group were observably higher compared with the celecoxib group (P < 0.05), and the inflammatory factor levels in the celecoxib group were remarkably higher compared with the iguratimod group (P < 0.05). Before treatment, no notable difference in the Lysholm scores was found among the three groups, and the patients’ knee joint function was gradually improved after treatment. To be specific, after 4 and 8 weeks of treatment, the iguratimod group had observably higher Lysholm scores compared with the other two groups (P < 0.05), and the celecoxib group had signally higher Lysholm scores compared with the diclofenac sodium group (P < 0.05). The iguratimod group got markedly lower Western Ontario and McMaster Universities (WOMAC) score compared with the celecoxib group (P < 0.05); Compared with the diclofenac sodium group, the celecoxib group got remarkably lower WOMAC score (P < 0.05). During treatment, few patients suffered from mild gastrointestinal discomfort and hepatic dysfunction in the three groups, and no other severe adverse reactions were found. No statistical difference in the total incidence of adverse reactions among the three groups was observed (P > 0.05). Conclusion: The combination of nonsteroidal anti-inflammatory drugs with platelet-rich plasma can further reduce the inflammatory reactions of the patients with osteoarthritis and improve their knee joint function. Significantly, the iguratimod, with high safety, has observably better effects on inhibiting inflammatory factors and improving knee joint function compared with diclofenac sodium and celecoxib.

Journal of healthcare engineering 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, Computed Properties of 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

Shen, Lan published the artcileSynthesis and structure-activity relationships of thiadiazole-derivatives as potent and orally active peroxisome proliferator-activated receptors α/δ dual agonists, Recommanded Product: 2,4-Dichlorobenzamide, the publication is Bioorganic & Medicinal Chemistry (2008), 16(6), 3321-3341, database is CAplus and MEDLINE.

Replacement of the methyl-thiazole moiety of GW501516 (a PPARδ selective agonist) with [1,2,4]thiadiazole gave compound 21 (I) which unexpectedly displayed submicromolar potency as a partial agonist at PPARα in addition to the high potency at PPARδ. A structure-activity relationships study of 21 resulted in the identification of 40 as a potent and selective PPARα/δ dual agonist. Compound 40 and its close analogs represent a new series of PPARα/δ dual agonists. The high potency, high selectivity, significant gene induction, excellent PK profiles, low P 450 inhibition or induction, and good in vivo efficacy in four animal models support 40 being selected as a pre-clin. study candidate, and may render 40 as a valuable pharmacol. tool in elucidating the complex roles of PPARα/δ dual agonists, and the potential usage for the treatment of metabolic syndrome.

Bioorganic & Medicinal Chemistry published new progress about 2447-79-2. 2447-79-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Amide, name is 2,4-Dichlorobenzamide, and the molecular formula is C30H32ClN7O2, Recommanded Product: 2,4-Dichlorobenzamide.

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

Jia, Ruoyu published the artcileEffect of Sacubitril/Valsartan on renal function in patients with chronic kidney disease and heart failure with preserved ejection fraction: A real-world 12-week study, Application In Synthesis of 137862-53-4, the publication is European Journal of Pharmacology (2022), 175053, database is CAplus and MEDLINE.

Patients with chronic kidney disease (CKD) are often complicated with heart failure with preserved ejection fraction (HFpEF). However, several drugs, including angiotensin-converting enzyme inhibitor (ACEI) and angiotensin receptor blocker (ARB), have not shown apparent benefits in terms of morbidity and mortality of HFpEF. PARAMOUNT and other studies have shown the potential benefits of Sacubitril/Valsartan on patients with HFpEF, but its effects on renal function and the effect of low-dose Sacubitril/Valsartan in actual clin. conditions have not been thoroughly evaluated. In our longitudinal and observational research, 353 patients were followed up for 12 wk. We evaluated renal function [urinary protein, serum creatinine and estimated glomerular filtration rate (eGFR)] and cardiac function [NT-proBNP (brain natriuretic peptide), New York Heart Association (NYHA) classification, left ventricular ejection fraction (LVEF), left atrial width and left ventricular end-diastolic width] at baseline and during follow-up. Worsening renal function (WRF) was defined as an increased serum creatinine≥26.5umol/L or decreased eGFR≥20%. The decline of eGFR in the Sacubitril/Valsartan group was slower than that in the control group (p = 0.021). The outcome of proteinuria in the ACEI/ARB group was significantly better than that in the Sacubitril/Valsartan group (p = 0.001). In terms of echocardiogram, the average left atrial width in Sacubitril/Valsartan group decreased by 1.38 ± 3.02 mm, which was significantly lower than that in the ACEI/ARB group (p = 0.02). The increase of urine protein class in the ACEI/ARB group increased the risk of WRF with statistical significance (OR = 2.36, 95%CI 1.01-5.49, p = 0.047), but no statistical significance was found in all the patients or Sacubitril/Valsartan group. In conclusion, Sacubitril/Valsartan could more effectively slow down renal function decline and reverse myocardial remodeling in patients with CKD and HFpEF than ACEI/ARB, even at low doses, though its protective effect on urinary protein is not as good as that of ACEI/ARB.

European Journal of Pharmacology published new progress about 137862-53-4. 137862-53-4 belongs to amides-buliding-blocks, auxiliary class GPCR/G Protein,Angiotensin Receptor, name is (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid, and the molecular formula is C24H29N5O3, Application In Synthesis of 137862-53-4.

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

Cheng, Dong-Bing published the artcileEndogenous Reactive Oxygen Species-Triggered Morphology Transformation for Enhanced Cooperative Interaction with Mitochondria, Product Details of C4H6F3NOS, the publication is Journal of the American Chemical Society (2019), 141(18), 7235-7239, database is CAplus and MEDLINE.

The morphol. controlled mol. assemblies play vital roles in biol. systems. Here we present endogenous reactive oxygen species (ROS)-triggered morphol. transformation of polymer-peptide conjugates (PPCs) for cooperative interaction with mitochondria, exhibiting high tumor therapeutic efficacy. The PPCs are composed of (i) a β-sheet-forming peptide KLVFF conjugated with poly(ethylene glycol) through ROS-cleavable thioketal, (ii) a mitochondria-targeting cytotoxic peptide KLAK, and (iii) a poly(vinyl alc.) backbone. The self-assembled PPCs nanoparticles can enter cells and target mitochondria. Because of overgenerated ROS around mitochondria in most cancer cells, the thioketal linker can be cleaved, leading to transformation from nanoparticles to fibrous nanostructures. As a result, the locational nanofibers with exposure of KLAK exhibit enhanced multivalent cooperative interactions with mitochondria, which causes selective cytotoxicity against cancer cells and powerful tumor suppression efficacy in vivo. As the first example of ROS-triggered intracellular transformation, the locational assembly strategy in vivo may provide a new insight for disease diagnosis and therapy through enhanced interaction with targeting site.

Journal of the American Chemical Society published new progress about 1869-45-0. 1869-45-0 belongs to amides-buliding-blocks, auxiliary class Trifluoromethylated Building Blocks, name is 2,2,2-Trifluoro-N-(2-mercaptoethyl)acetamide, and the molecular formula is C4H6F3NOS, Product Details of C4H6F3NOS.

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

Fan, Wei published the artcileIncreasing time on target: utilization of inhibitors of cysteine cathepsins to enhance the tumor retention of receptor-targeted agents, Application In Synthesis of 2418-95-3, the publication is Chemical Communications (Cambridge, United Kingdom) (2018), 54(80), 11268-11271, database is CAplus and MEDLINE.

We report a strategy of utilizing irreversible cysteine cathepsin inhibitor as trapping agent to increase the tumor residence time of receptor-targeted agents. The targeted constructs incorporating these cysteine cathepsin trapping agents were able to form high mol. weight adducts with intracellular cysteine cathepsins, thus achieving superior retention in tumor tissues.

Chemical Communications (Cambridge, United Kingdom) published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C11H22N2O4, Application In Synthesis of 2418-95-3.

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

Wu, Yue-Ming published the artcileFacile synthesis of high molecular weight polypeptides via fast and moisture insensitive polymerization of alpha-amino acid N-carboxyanhydrides, Category: amides-buliding-blocks, the publication is Chinese Journal of Polymer Science (2020), 38(10), 1131-1140, database is CAplus.

Polypeptides have been widely utilized in the fields of biomaterials and biomedicine. Ever since N-carboxyanhydride (NCA) was reported by Hermann Leuchs in 1906, ring-opening polymerization of NCAs has been extensively used to prepare polypeptides. Despite continuous innovations, it is still challenging to synthesize polypeptides in high mol. weight efficiently. To address this challenge, we developed KHMDS/NaHMDS initiated fast NCA polymerization that is also moisture tolerant, open-flask amenable and terminal tunable. This NCA polymerization was able to proceed in most common solvents and meet the solubility requirement of variable NCA monomers and corresponding polypeptides. KHMDS can initiate γ-benzyl-L-glutamate-N-carboxyanhydride (BLG NCA) polymerization in a reaction rate 92 times faster than does hexylamine and 80 times faster than does triethylamine. This NCA polymerization also demonstrated easy and fast synthesis of gram-scale long chain polypeptides in an open flask.

Chinese Journal of Polymer Science published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C7H6Cl2, Category: amides-buliding-blocks.

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

Tu, Shun published the artcileN-(3-cyano-1H-indol-5-yl)isonicotinamide and N-(3-cyano-1H-indol-5-yl)-1H-benzo[d]imidazole-5-carboxamide derivatives: Novel amide-based xanthine oxidase inhibitors, Synthetic Route of 1453-82-3, the publication is Bioorganic Chemistry (2021), 105181, database is CAplus and MEDLINE.

Our previous work demonstrated that amide is an efficient linker to explore chem. space of xanthine oxidase (XO) inhibitors that are entirely different from febuxostat and topiroxostat. In this effort, with 3-cyano-1H-indol-5-yl as a key moiety, two series of amide-based XO inhibitors, N-(3-cyano-1H-indol-5-yl)isonicotinamides and N-(3-cyano-1H-indol-5-yl)-1H-benzo[d]imidazole-5-carboxamides, were designed and synthesized. The structure-activity relationship investigation identified N-(3-cyano-1-cyclopentyl-1H-indol-5-yl)-1H-benzo[d]imidazole-5-carboxamide (I, IC₅₀ = 0.62μM) as the most promising compound, with 14.4-fold higher in vitro inhibitory potency than allopurinol (IC₅₀ = 8.91μM). Mol. simulations provided reasonable interaction modes for the representative compounds Furthermore, in vivo activity evaluation demonstrated that compound I (oral dose of 12.8 mg/kg) has obviously hypouricemic effect on a potassium oxonate induced hyperuricemic rat model. Cytotoxicity assay and ADME prediction also supported that I is an excellent lead for further exploration of amide-based XO inhibitors.

Bioorganic Chemistry published new progress about 1453-82-3. 1453-82-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is Isonicotinamide, and the molecular formula is C17H28ClNO3, Synthetic Route of 1453-82-3.

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