Month: October 2022

Maines, Lynn W.; Fitzpatrick, Leo R.; French, Kevin J.; Zhuang, Yan; Xia, Zuping; Keller, Staci N.; Upson, John J.; Smith, Charles D. published the artcile< Suppression of Ulcerative Colitis in Mice by Orally Available Inhibitors of Sphingosine Kinase>, Computed Properties of 6054-98-4, the main research area is sphingosine kinase ABC294640 ABC747080 ulcerative colitis anticolitis antiinflammatory signaling.

A critical step in the mechanism of action of inflammatory cytokines is the stimulation of sphingolipid metabolism, including activation of sphingosine kinase (SK), which produces the mitogenic and proinflammatory lipid sphingosine 1-phosphate (S1P). We have developed orally bioavailable compounds that effectively inhibit SK activity in vitro in intact cells and in cancer models in vivo. In this study, we assessed the effects of these SK inhibitors on cellular responses to tumor necrosis factor alpha (TNFα) and evaluated their efficacy in the dextran sulfate sodium (DSS) model of ulcerative colitis in mice. Using several cell systems, it was shown that the SK inhibitors block the ability of TNFα to activate nuclear factor kappa B (NFκB), induce expression of adhesion proteins, and promote production of prostaglandin E2 (PGE2). In an acute model of DSS-induced ulcerative colitis, SK inhibitors were equivalent to or more effective than Dipentum in reducing disease progression, colon shortening, and neutrophil infiltration into the colon. The effects of SK inhibitors were associated with decreased colonic levels of inflammatory cytokines TNFα, interleukin (IL)-1β, interferon gamma (IFN)-γ, IL-6, and reduction of S1P levels. A similar reduction in disease progression was provided by SK inhibitors in a chronic model of ulcerative colitis in which the mice received 3-wk-long cycles of DSS interspaced with week-long recovery periods. In the chronic model, immunohistochem. for SK showed increased expression in DSS-treated mice (compared with water-treated controls) that was reduced by drug treatment. S1P levels were also elevated in the DSS group and significantly reduced by drug treatment. Together, these data indicate that SK is a critical component in inflammation and that inhibitors of this enzyme may be useful in treating inflammatory bowel diseases.

Digestive Diseases and Sciences published new progress about Anti-inflammatory agents. 6054-98-4 belongs to class alcohols-buliding-blocks, and the molecular formula is C14H8N2Na2O6, Computed Properties of 6054-98-4.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Kato, Yuichi; Inoue, Tomoka; Furuyama, Yuuki; Ohgane, Kenji; Sadaie, Mahito; Kuramochi, Kouji published the artcile< Deoxygenation of tertiary and secondary alcohols with sodium borohydride, trimethylsilyl chloride, and potassium iodide in acetonitrile>, Recommanded Product: Triphenylmethanol, the main research area is alkane preparation; tertiary secondary alc deoxygenation.

In this study, a deoxygenation method was developed for tertiary and secondary alcs., ROH [R = triphenylmethyl, 9-phenyl-9H-xanthen-9-yl, bis(4-methoxyphenyl)(thiophen-2-yl)methyl, etc.] using trimethylsilane and trimethylsilyl iodide generated in situ from sodium borohydride and trimethylsilyl chloride, and trimethylsilyl chloride and potassium iodide, resp. In this method, tertiary and secondary alcs., which provided stable carbocations, were converted into the corresponding alkanes RH. This paper also presents the optimization of the reaction conditions, the reaction mechanism, as well as the scope and limitations of the method.

Tetrahedron Letters published new progress about Alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 76-84-6 belongs to class alcohols-buliding-blocks, and the molecular formula is C19H16O, Recommanded Product: Triphenylmethanol.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Wei, Duo; Dorcet, Vincent; Darcel, Christophe; Sortais, Jean-Baptiste published the artcile< Synthesis of Quinolines Through Acceptorless Dehydrogenative Coupling Catalyzed by Rhenium PN(H)P Complexes>, Application In Synthesis of 403-41-8, the main research area is quinoline preparation green chem; aryl alc hydroxymethyl aniline dehydrogenative coupling rhenium catalyst; ketone hydroxymethyl aniline dehydrogenative coupling rhenium catalyst; nitrile hydroxymethyl aniline dehydrogenative coupling rhenium catalyst; annulation; dehydrogenative coupling; hydrogen borrowing; quinoline; rhenium.

The practical and sustainable synthesis of substituted quinolines I (R1 = C6H5, cyclopropyl, NH2, etc.; R2 = H, C6H5, CH3, etc.; R1R2 = (CH2)4, (CH2)6) and 5,6-dihydro-benzo[c]acridine was achieved through the annulation of 2-aminobenzyl alc. with various secondary alcs. R1CH(OH)CH2R2, ketones R1C(O)CH2R2, phenylacetaldehyde, or nitriles R2CH2CN, under hydrogen-borrowing conditions. Under the catalysis of well-defined rhenium complexes bearing tridentate diphosphinoamino ligands, the reaction proceeded efficiently (31 examples were isolated with yields up to 96%) for affording a variety of quinoline derivatives I and 5,6-dihydro-benzo[c]acridine.

ChemSusChem published new progress about Aromatic alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 403-41-8 belongs to class alcohols-buliding-blocks, and the molecular formula is C8H9FO, Application In Synthesis of 403-41-8.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Magre, Marc; Paffenholz, Eva; Maity, Bholanath; Cavallo, Luigi; Rueping, Magnus published the artcile< Regiodivergent Hydroborative Ring Opening of Epoxides via Selective C-O Bond Activation>, Quality Control of 403-41-8, the main research area is secondary tertiary alc regiodivergent synthesis hydroborative ring opening epoxide.

A magnesium-catalyzed regiodivergent C-O bond cleavage protocol is presented. Readily available magnesium catalysts achieve the selective hydroboration of a wide range of epoxides and oxetanes yielding secondary and tertiary alcs. in excellent yields and regioselectivities. Exptl. mechanistic investigations and DFT calculations provide insight into the unexpected regiodivergence and explain the different mechanisms of the C-O bond activation and product formation.

Journal of the American Chemical Society published new progress about C-O bond activation. 403-41-8 belongs to class alcohols-buliding-blocks, and the molecular formula is C8H9FO, Quality Control of 403-41-8.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Hartogh, Danja J. Den; Tsiani, Evangelia published the artcile< Health benefits of resveratrol in kidney disease: evidence from in vitro and in vivo studies>, Name: (E)-5-(4-Hydroxystyryl)benzene-1,3-diol, the main research area is resveratrol kidney disease health benefit review; fibroblasts; glomerulosclerosis; kidney disease; mesangial cells; renal cancer; renal epithelial cells; resveratrol.

A review. Different diseases and disorders that affect the kidneys include, but are not limited to, glomerulonephritis, diabetic nephropathy, polycystic kidney disease, kidney stones, renal fibrosis, sepsis, and renal cell carcinoma. Kidney disease tends to develop over many years, making it difficult to identify until much later when kidney function is severely impaired and undergoing kidney failure. Although conservative care, symptom management, medication, dialysis, transplantation, and aggressive renal cancer therapy are some of the current strategies/approaches to kidney disease treatment, new preventative targeted therapies are needed. Epidemiol. studies have suggested that a diet rich in fruits and vegetables is associated with health benefits including protection against kidney disease and renal cancer. Resveratrol, a polyphenol found in grapes and berries, has been reported to have antioxidant, anti-inflammatory, antidiabetic, hepatoprotective, neuroprotective, and anti-cancer properties. The current review summarizes the existing in vitro and in vivo animal and human studies examining the nephroprotective effects of resveratrol.

Nutrients published new progress about Kidney disease. 501-36-0 belongs to class alcohols-buliding-blocks, and the molecular formula is C14H12O3, Name: (E)-5-(4-Hydroxystyryl)benzene-1,3-diol.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Singh, Ashima; Gupta, Shruti; Khurana, Jitender M. published the artcile< Zinc Chloride Mediated Nucleophilic Substitution: Amination and Thioetherification of Alcohols at Room Temperature>, SDS of cas: 76-84-6, the main research area is zinc chloride catalyst nucleophilic substitution amination thioetherification alc.

The authors report a high yielding, waste-free, efficient synthesis of thioethers and amines from secondary or tertiary alcs. and anilines or thiophenols in dichloromethane in the presence of ZnCl2 at room temperature

Organic Preparations and Procedures International published new progress about Alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 76-84-6 belongs to class alcohols-buliding-blocks, and the molecular formula is C19H16O, SDS of cas: 76-84-6.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Uehara, Tomoya; Kanazawa, Naoki; Suzuki, Chie; Mizuno, Yuki; Suzuki, Hiroyuki; Hanaoka, Hirofumi; Arano, Yasushi published the artcile< Renal Handling of 99mTc-Labeled Antibody Fab Fragments with a Linkage Cleavable by Enzymes on Brush Border Membrane>, Related Products of 76-84-6, the main research area is technetium 99m Fab fragment linkage cleavage renal brush border.

The high and persistent renal radioactivity levels after injection of radiolabeled low-mol.-weight polypeptides constitute a significant problem for their diagnostic and therapeutic applications, especially when they are labeled with metallic radionuclides. To improve the renal radioactivity levels of technetium-99m (99mTc)-labeled Fab fragments, a mercaptoacetyltriglycine (MAG3)-based new bifunctional chelating agent with a cleavable glycyl-phenylalanyl-lysine (GFK) linkage, MAG3-GFK-suc-TFP, was designed, synthesized, and evaluated. 99mTc-labeled Fab was obtained by reacting MAG3-GFK-Fab conjugate with 99mTc-glucarate. The GFK linkage remained stable in plasma but was cleaved by enzymes on the renal brush border membrane. The comparative biodistribution studies with indium-111 (111In)-labeled Fab using SCN-CHX-A”-DTPA showed that while both radiolabeled Fabs exhibited similar elimination rates from the blood, [99mTc]Tc-MAG3-GFK-Fab registered much lower renal radioactivity levels from 30 min post-injection onward due to the release and subsequent urinary excretion of [99mTc]Tc-MAG3-Gly. However, [99mTc]Tc-MAG3-GFK-Fab showed an increase in the intestinal radioactivity levels with the time that was not observed with 111In-labeled Fab. The anal. of the intestinal contents suggested the redistribution of [99mTc]Tc-MAG3-Gly to the intestine. The retrospective comparison of [99mTc]Tc-MAG3-GFK-Fab with the radiolabeled Fabs so far prepared under the identical concept suggested that some portion of [99mTc]Tc-MAG3-Gly was generated after the coated vesicle formation and they were excreted into the blood, and subsequently redistributed in the intestine via hepatobiliary excretion. In conclusion, MAG3-GFK-suc-TFP provided 99mTc-labeled Fabs that exhibit low renal radioactivity shortly after injection by the post-labeling procedure. The present study indicated that, contrary to our earlier proposal, the generation of the radiometabolites would proceed not only during the internalization process of the parental antibody fragments but also after coated vesicle formation. This study also showed that the intracellular behaviors of radiometabolites played crucial roles in the elimination rates and the routes of the radioactivity from the kidney.

Bioconjugate Chemistry published new progress about Brush border. 76-84-6 belongs to class alcohols-buliding-blocks, and the molecular formula is C19H16O, Related Products of 76-84-6.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Bernstein, Charles N.; Nugent, Zoann; Blanchard, James F. published the artcile< 5-Aminosalicylate Is Not Chemoprophylactic for Colorectal Cancer in IBD: A Population Based Study>, Recommanded Product: Sodium 5,5′-(diazene-1,2-diyl)bis(2-hydroxybenzoate), the main research area is Asacol chemopreventive agent prophylaxis colorectal cancer inflammatory bowel disease.

OBJECTIVES: We aimed to determine if use of 5-aminosalicylates (5-ASA) was associated with a reduced risk of colorectal cancer (CRC) in people with inflammatory bowel disease (IBD). METHODS: We used the population-based University of Manitoba IBD Epidemiol. Database that tracks all health-care visits from 1984 to 2008 of all Manitobans with IBD and all prescription medication use since 1995. In 2008, there were 8,744 subjects with IBD (ulcerative colitis 4,325, Crohn’s disease 4,419, females 4,851, males 3,893). In study I, we assessed the incidence of CRC among 5-ASA users (≥1 yr, ≥5 years of cumulative use) compared with nonusers. In study II, we assessed a cohort of those with CRC (n=101) diagnosed in 1995-2008, matched to a control cohort by age, sex, disease duration, and disease diagnosis without CRC (n=303), and logistic anal. was undertaken. RESULTS: For study I, the hazard ratio for CRC among 5-ASA users was 1.04 (95% confidence interval (CI) 0.67-1.62, P=0.87) at ≥1 yr of use and 2.01 (95% CI 1.04-3.9, P=0.038) at ≥5 years of use with no difference when assessing by diagnosis. Males, but not females, using 5-ASA for ≥5 years had an increased risk of CRC. In study II, CRC cases had similar use of any 5-ASA compared with controls for ≥1 yr of use (1.02, 95% CI 0.60-1.74) or ≥5 years (1.96, 95% CI 0.84-4.55), and a similar mean number of 5-ASA prescriptions at 10 vs. 11 (P=0.8) and a similar mean number of dose days at 330 vs. 410 (P=0.69). CONCLUSIONS: Our results support the majority of studies to date that 5-ASA is not chemoprophylactic in IBD for CRC. Am J Gastroenterol 2011; 106:731-736; doi:10.1038/ajg.2011.50; published online 15 March 2011.

American Journal of Gastroenterology published new progress about Colorectal neoplasm. 6054-98-4 belongs to class alcohols-buliding-blocks, and the molecular formula is C14H8N2Na2O6, Recommanded Product: Sodium 5,5′-(diazene-1,2-diyl)bis(2-hydroxybenzoate).

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Grinan-Ferre, Christian; Bellver-Sanchis, Aina; Izquierdo, Vanessa; Corpas, Ruben; Roig-Soriano, Joan; Chillon, Miguel; Andres-Lacueva, Cristina; Somogyvari, Milan; Soti, Csaba; Sanfeliu, Coral; Pallas, Merce published the artcile< The pleiotropic neuroprotective effects of resveratrol in cognitive decline and Alzheimer′s disease pathology: From antioxidant to epigenetic therapy>, Reference of 501-36-0 , the main research area is review cognitive decline alzheimer disease neuroprotective antioxidant epigenetic resveratrol; Antioxidants; Epigenetic; Gut microbiota; Klotho; Neurodegeneration; Resveratrol; Senescence.

A review. While the elderly segment of the population continues growing in importance, neurodegenerative diseases in crease exponentially. Lifestyle factors such as nutrition, exercise, and education, among others, influence ageing progression, throughout life. Notably, the Central Nervous System (CNS) can benefit from nutritional strategies and dietary interventions that prevent signs of senescence, such as cognitive decline or neurodegenerative dis eases such as Alzheimer′s disease and Parkinson′s Disease. The dietary polyphenol Resveratrol (RV) possesses antioxidant and cytoprotective effects, producing neuroprotection in several organisms. The (OS) occurs because of (ROS) accumulation that has been proposed to explain the cause of the ageing. One of the most harmful effects of ROS in the cell is DNA damage. Nevertheless, there is also evidence demonstrating that OS can produce other mol. changes such as mitochondrial dysfunction, inflammation, apoptosis, and epigenetic modifications, among others. Interestingly, the dietary polyphenol RV is a potent antioxidant and possesses pleiotropic actions, exerting its activity through various mol. pathways. In this review, we give a comprehensive overview of the main mechanisms of action of RV in different exptl. models, including clin. trials and discuss how the interconnection of these mol. events could explain the neuroprotective effects induced by RV.

Ageing Research Reviews published new progress about Accelerated aging disorder. 501-36-0 belongs to class alcohols-buliding-blocks, and the molecular formula is C14H12O3, Reference of 501-36-0 .

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts