Tag: 100-200

On January 15, 2021, Kaniusaite, Milda; Tailhades, Julien; Kittilae, Tiia; Fage, Christopher D.; Goode, Robert J. A.; Schittenhelm, Ralf B.; Cryle, Max J. published an article.Synthetic Route of 32462-30-9 The title of the article was Understanding the early stages of peptide formation during the biosynthesis of teicoplanin and related glycopeptide antibiotics. And the article contained the following:

The biosynthesis of the glycopeptide antibiotics (GPAs) demonstrates the exceptional ability of nonribosomal peptide (NRP) synthesis to generate diverse and complex structures from an expanded array of amino acid precursors. While the heptapeptide cores of GPAs share a conserved C terminus, including the aromatic residues involved crosslinking and that are essential for the antibiotic activity of GPAs, most structural diversity is found within the N terminus of the peptide. Furthermore, the origin of the (D)-stereochem. of residue 1 of all GPAs is currently unclear, despite its importance for antibiotic activity. Given these important features, we have now reconstituted modules (M) 1-4 of the NRP synthetase (NRPS) assembly lines that synthesize the clin. relevant type IV GPA teicoplanin and the related compound A40926. Our results show that important roles in amino acid modification during the NRPS-mediated biosynthesis of GPAs can be ascribed to the actions of condensation domains present within these modules, including the incorporation of (D)-amino acids at position 1 of the peptide. Our results also indicate that hybrid NRPS assembly lines can be generated in a facile manner by mixing NRPS proteins from different systems and that uncoupling of peptide formation due to different rates of activity seen for NRPS modules can be controlled by varying the ratio of NRPS modules. Taken together, this indicates that NRPS assembly lines function as dynamic peptide assembly lines and not static megaenzyme complexes, which has significant implications for biosynthetic redesign of these important biosynthetic systems. The experimental process involved the reaction of H-Phg(4-OH)-OH(cas: 32462-30-9).Synthetic Route of 32462-30-9

The Article related to nonribosomal peptide synthetase teicoplanin biosynthesis stereochem glycopeptide antibiotic, biosynthesis, epimerisation, glycopeptide antibiotics, nonribosomal peptide synthetase, teicoplanin and other aspects.Synthetic Route of 32462-30-9

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On August 9, 2021, Sun, Han; Xie, Xiaoxin; Huang, Qiu; Wang, Zhaoxu; Chen, Kejun; Li, Xiaolei; Gao, Jian; Li, Yutao; Li, Hong; Qiu, Jieshan; Zhou, Weidong published an article.Category: alcohols-buliding-blocks The title of the article was Fluorinated Poly-oxalate Electrolytes Stabilizing both Anode and Cathode Interfaces for All-Solid-State Li/NMC811 Batteries. And the article contained the following:

The relatively narrow electrochem. steady window and low ionic conductivity are two critical challenges for Li+-conducting solid polymer electrolytes (SPE). Here, a family of poly-oxalate(POE) structures were prepared as SPE; among them, POEs composed from diols with an odd number of carbons show higher ionic conductivity than those composed from diols with an even number of carbons, and the POE composed from propanediol (C5-POE) has the highest Li+ conductivity The HOMO (HOMO) electrons of POE were found located on the terminal units. When using trifluoroacetate as the terminating unit (POE-F), not only does the HOMO become more neg., but also the HOMO electrons shift to the middle oxalate units, improving the antioxidative capability. Furthermore, the interfacial compatibility across the Li-metal/POE-F is also improved by the generation of a LiF-based solid-electrolyte-interlayer(SEI). With the trifluoroacetate-terminated C5-POE (C5-POE-F) as the electrolyte and Li+-conducting binder in the cathode, the all-solid-state Li/LiNi0.8Mn0.1Co0.1O2(NMC811) cells showed significantly improved stability than the counterpart with poly-ether, providing a promising candidate for the forthcoming all-solid-state high-voltage Li-metal batteries. The experimental process involved the reaction of Pentane-1,5-diol(cas: 111-29-5).Category: alcohols-buliding-blocks

The Article related to lithium nmc811 transesterification polycondensation process elec thermal morphol property, all-solid-state batteries, eutectic phenomenon, high-voltage cells, interfaces, polymer electrolytes and other aspects.Category: alcohols-buliding-blocks

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On September 21, 2020, Prabakaran, Rajalakshmi; Marie, J. Margaret; Xavier, A. John Maria published an article.Electric Literature of 111-29-5 The title of the article was Biobased Unsaturated Polyesters Containing Castor Oil-Derived Ricinoleic Acid and Itaconic Acid: Synthesis, In Vitro Antibacterial, and Cytocompatibility Studies. And the article contained the following:

A set of antibacterial polyesters, with inherent multibiomedical properties, comprising biobased monomers such as ricinoleic acid and itaconic acid together with α,ω-aliphatic diols, were synthesized via a greener synthetic route. The structures of the synthesized biobased unsaturated polyesters were confirmed by Fourier transform IR and NMR spectral studies. The mol. weight of the prepolymers was determined by gel permeation chromatog. anal. The cured polymeric membranes were structurally characterized by attenuated total reflection IR and powder X-ray diffraction. The mech., thermal, wettability, swelling, and sol content measurements of the cured polyester membranes were studied. The synthesized polyesters showed significant antibacterial activity against the Gram-pos. bacteria, Staphylococcus aureus. The polyesters IRPe, IRD, and IRDd had shown potent anticancer activity against human liver cancer HepG2 cells and human breast cancer MCF7 cells. The highly hydrophilic IRH polyester was tested for its cell adhesive nature in mouse fibroblast cells (L929). The hydrophilicity, slow in vitro degradability, and cell adhesive capacity favor the exploration of these polymers further as drug carriers or as scaffolds for tissue engineering applications. The antibacterial and anticancer activities together with compatibility in normal human kidney embryonic Hek 293 cells exhibit the potentiality of these polymeric biomaterials to find application as anticancer drugs and antibacterial agents. The experimental process involved the reaction of Pentane-1,5-diol(cas: 111-29-5).Electric Literature of 111-29-5

The Article related to polyester ricinoleic itaconic acid antibacterial antitumor, antibacterial unsaturated polyesters, anticancer activity, biocompatible, biodegradable, castor oil, itaconic acid, ricinoleic acid and other aspects.Electric Literature of 111-29-5

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On June 3, 2022, Bolduc, Trevor G.; Lee, Cayo; Chappell, William P.; Sammis, Glenn M. published an article.Synthetic Route of 143-10-2 The title of the article was Thionyl fluoride-mediated one-pot substitutions and reductions of carboxylic acids. And the article contained the following:

Thionyl fluoride (SOF2) is an underutilized reagent that is yet to be extensively studied for its synthetic applications. We previously reported that it is a powerful reagent for both the rapid syntheses of acyl fluorides and for one-pot peptide couplings, but the full scope of these nucleophilic acyl substitutions had not been explored. Herein, we report one-pot thionyl fluoride-mediated syntheses of peptides and amides (35 examples, 45-99% yields) that were not explored in our previous study. The scope of thionyl fluoride-mediated nucleophilic acyl substitutions was also expanded to encompass esters (24 examples, 64-99% yields) and thioesters (11 examples, 24-96% yields). In addition, we demonstrate that the scope of thionyl fluoride-mediated one-pot reactions can be extended beyond nucleophilic acyl substitutions to mild reductions of carboxylic acids using NaBH4 (13 examples, 33-80% yields). The experimental process involved the reaction of 1-Decanethiol(cas: 143-10-2).Synthetic Route of 143-10-2

The Article related to peptide amide one pot synthesis thionyl fluoride mediated thioester, carboxylic acid nucleophilic acyl substitution reduction thionyl fluoride mediated, amino acid peptide coupling protection and other aspects.Synthetic Route of 143-10-2

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On December 31, 2020, Ulaszewska, Maria M.; Koutsos, Athanasios; Trost, Kajetan; Stanstrup, Jan; Garcia-Aloy, Mar; Scholz, Matthias; Fava, Francesca; Natella, Fausta; Scaccini, Cristina; Vrhovsek, Urska; Tuohy, Kieran; Lovegrove, Julie; Mattivi, Fulvio published an article.Electric Literature of 621-37-4 The title of the article was Two apples a day modulate human:microbiome co-metabolic processing of polyphenols, tyrosine and tryptophan.. And the article contained the following:

Methods: Using an untargeted metabolomics approach, we aimed to identify biomarkers of long-term apple intake and explore how apples impact on the human plasma and urine metabolite profiles. Forty mildly hypercholesterolemic volunteers consumed two whole apples or a sugar and energy-matched control beverage, daily for 8 wk in a randomized, controlled, crossover intervention study. The metabolome in plasma and urine samples was analyzed via untargeted metabolomics. Results: We found 61 urine and 9 plasma metabolites being statistically significant after the whole apple intake compared to the control beverage, including several polyphenol metabolites that could be used as BFIs. Furthermore, we identified several endogenous indole and phenylacetyl-glutamine microbial metabolites significantly increasing in urine after apple consumption. The multiomic dataset allowed exploration of the correlations between metabolites modulated significantly by the dietary intervention and fecal microbiota species at genus level, showing interesting interactions between Granulicatella genus and phenyl-acetic acid metabolites. Phloretin glucuronide and phloretin glucuronide sulfate appeared promising biomarkers of apple intake; however, robustness, reliability and stability data are needed for full BFI validation. Conclusion: The identified apple BFIs can be used in future studies to assess compliance and to explore their health effects after apple intake. The experimental process involved the reaction of 3-Hydroxyphenylacetic acid(cas: 621-37-4).Electric Literature of 621-37-4

The Article related to apple biomarker polyphenol tyrosine tryptophan microbiome metabolic process, apples, biomarker of food intake, orbitrap, polyphenols, tryptophan, tyrosine, untargeted metabolomics, validation and other aspects.Electric Literature of 621-37-4

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On September 14, 2017, Bollinger, Katrina A.; Felts, Andrew S.; Brassard, Christopher J.; Engers, Julie L.; Rodriguez, Alice L.; Weiner, Rebecca L.; Cho, Hyekyung P.; Chang, Sichen; Bubser, Michael; Jones, Carrie K.; Blobaum, Anna L.; Niswender, Colleen M.; Conn, P. Jeffrey; Emmitte, Kyle A.; Lindsley, Craig W. published an article.Related Products of 386704-04-7 The title of the article was Design and Synthesis of mGlu2 NAMs with Improved Potency and CNS Penetration Based on a Truncated Picolinamide Core. And the article contained the following:

Herein, the authors detail the optimization of the mGlu2 neg. allosteric modulator (NAM), 4-(4-fluorophenyl)-5-((1-methyl-1H-pyrazol-3-yl)methoxy)picolinamide (VU6001192), by a reductionist approach to afford a novel, simplified mGlu2 NAM scaffold. This new chemotype not only affords potent and selective mGlu2 inhibition, as exemplified by VU6001966 (mGlu2 IC50 = 78 nM, mGlu3 IC50 > 30 μM), but also excellent central nervous system (CNS) penetration (Kp = 1.9, Kp,uu = 0.78), a feature devoid in all previously disclosed mGlu2 NAMs (Kps ≈ 0.3, Kp,uus ≈ 0.1). Moreover, this series, based on overall properties, represents an exciting lead series for potential mGlu2 PET tracer development. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Related Products of 386704-04-7

The Article related to mglu2 central nervous system penetration picolinamide pharmacokinetics, cns penetration, negative allosteric modulator (nam), vu6001966, depression, metabotropic glutamate receptor 2 (mglu2) and other aspects.Related Products of 386704-04-7

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On May 31, 1989, Young, Robert N.; Zamboni, Robert; Gauthier, Jacques Y.; Belley, Michel L. published a patent.Formula: C9H10O2 The title of the patent was Quinoline diacid derivatives useful as leukotriene antagonists, and their pharmaceutical compositions and use in medicaments. And the patent contained the following:

Title compounds I [R1 = H, halo, alkyl, alkenyl, alkynyl, CF3, SR2, S(O)R2, S(O)2R2, NR3R3, OR3, CO2R3, COR3, C(OH)R3R3, cyano,NO2, N3, (un)substituted Ph, PhCH2, PhCH2CH2, pyridyl; R2 = alkyl, alkenyl, alkynyl, CF3, (un)substituted Ph, PhCH2, PhCH2CH2; R3 = H, R2; R4 = H, halo, NO2, N3, cyano, SR2, NR3R3, OR3, alkyl, COR3; R5 = H, alkyl; Y = CR3:CR3, C:C, CO, NR3CO, CONR3, O, S, NR3, etc.; X1, X2 = complex chains, 1 or both containing C6H4, pyridine, or thiophene nucleus; Q1, Q2 = CO2R3, tetrazole, cyano, CHO, CH2OH, COCH2OH, etc.] are prepared for use as leukotriene antagonists (no data), and thereby as antiasthmatic, antiallergic, antiinflammatory, and cytoprotective agents. Thus, Wittig reaction of Me 2-[3-[2-(methoxycarbonyl)ethylthio]-3-(3-formylphenyl)propyl]benzoate (prepared in 6 steps) with [(7-chloroquinolin-2-yl)methyl]triphenylphosphonium bromide using BuLi in THF, and basic hydrolysis and salification of the product, gave [[[(chloroquinolinyl)ethenyl]phenyl](carboxyethylthio)propyl]benzoic acid di-Na salt II. The experimental process involved the reaction of Isochroman-3-ol(cas: 42900-89-0).Formula: C9H10O2

The Article related to quinoline preparation leukotriene antagonist, antiasthmatic quinoline preparation, antiallergic quinoline preparation, antiinflammatory quinoline preparation, antiulcer quinoline preparation and other aspects.Formula: C9H10O2

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On April 30, 2022, Li, Kun-Ping; Yuan, Min; Wu, Yong-Lin; Pineda, Miguel; Zhang, Chu-Mei; Chen, Yan-Fen; Chen, Zhi-quan; Rong, Xiang-Lu; Turnbull, Jeremy E.; Guo, Jiao published an article.Synthetic Route of 473-81-4 The title of the article was A High-Fat High-Fructose Diet Dysregulates the Homeostatic Crosstalk Between Gut Microbiome, Metabolome, and Immunity in an Experimental Model of Obesity. And the article contained the following:

Ample evidence supports the prominent role of gut-liver axis in perpetuating pathol. networks of high-fat high-fructose (HFF) diet induced metabolic disorders, however, the mol. mechanisms are still not fully understood. Herein, this study aims to present a holistic delineation and scientific explanation for the crosstalk between the gut and liver, including the potential mediators involved in orchestrating the metabolic and immune systems. An exptl. obesity-associated metaflammation rat model is induced with a HFF diet. An integrative multi-omics anal. is then performed. Following the clues illustrated by the multi-omics discoveries, putative pathways are subsequently validated by RT-qPCR and Western blotting. HFF diet leads to obese phenotypes in rats, as well as histopathol. changes. Integrated omics anal. shows that there exists a strong interdependence among gut microbiota composition, intestinal metabolites, and innate immunity regulation in the liver. Some carboxylic acids may contribute to gut-liver communication. Moreover, activation of the hepatic LPS-TLR4 pathway in obesity is confirmed. HFF-intake disturbs gut flora homeostasis. Crosstalk between gut microbiota and innate immune system mediates hepatic metaflammation in obese rats, associated with LPS-TLR4 signaling pathway activation. Moreover, α-hydroxyisobutyric acid and some other organic acids may play a role as messengers in the liver-gut axis. The experimental process involved the reaction of 2,3-Dihydroxypropanoic acid(cas: 473-81-4).Synthetic Route of 473-81-4

The Article related to high fructose diet gut microbiome metabolome immunity obesity, lps-tlr4, chronic inflammation, gut microbiota, innate immune system, integrated multi-omics analysis, α-hydroxyisobutyric acid and other aspects.Synthetic Route of 473-81-4

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Chandra, Pallavi; He, Li; Zimmerman, Matthew; Yang, Guozhe; Koster, Stefan; Ouimet, Mireille; Wang, Han; Moore, Kathyrn J.; Dartois, Veronique; Schilling, Joel D.; Philips, Jennifer A. published an article in 2020, the title of the article was Inhibition of fatty acid oxidation promotes macrophage control of Mycobacterium tuberculosis.Name: H-Phg(4-OH)-OH And the article contains the following content:

Macrophage activation involves metabolic reprogramming to support antimicrobial cellular functions. How these metabolic shifts influence the outcome of infection by intracellular pathogens remains incompletely understood. Mycobacterium tuberculosis (Mtb) modulates host metabolic pathways and utilizes host nutrients, including cholesterol and fatty acids, to survive within macrophages. We found that intracellular growth of Mtb depends on host fatty acid catabolism: when host fatty acid β-oxidation (FAO) was blocked chem. with trimetazidine, a compound in clin. use, or genetically by deletion of the mitochondrial fatty acid transporter carnitine palmitoyltransferase 2 (CPT2), Mtb failed to grow in macrophages, and its growth was attenuated in mice. Mechanistic studies support a model in which inhibition of FAO generates mitochondrial reactive oxygen species, which enhance macrophage NADPH oxidase and xenophagy activity to better control Mtb infection. Thus, FAO inhibition promotes key antimicrobial functions of macrophages and overcomes immune evasion mechanisms of Mtb. The experimental process involved the reaction of H-Phg(4-OH)-OH(cas: 32462-30-9).Name: H-Phg(4-OH)-OH

The Article related to fatty acid oxidation inhibition macrophage mitochondria tuberculosis, mycobacterium tuberculosis , nadph oxidase, fatty acid oxidation, innate immunity, macrophages, mitochondrial metabolism and other aspects.Name: H-Phg(4-OH)-OH

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Dias, Patricia; Pourova, Jana; Voprsalova, Marie; Nejmanova, Iveta; Mladenka, Premysl published an article in 2022, the title of the article was 3-Hydroxyphenylacetic Acid: A Blood Pressure-Reducing Flavonoid Metabolite.Category: alcohols-buliding-blocks And the article contains the following content:

Regular intake of polyphenol-rich food has been associated with a wide variety of beneficial health effects, including the prevention of cardiovascular diseases. However, the parent flavonoids have mostly low bioavailability and, hence, their metabolites have been hypothesized to be bioactive. One of these metabolites, 3-hydroxyphenylacetic acid (3-HPAA), formed by the gut microbiota, was previously reported to exert vasorelaxant effects ex vivo. The aim of this study was to shed more light on this effect in vivo, and to elucidate the mechanism of action. 3-HPAA gave rise to a dose-dependent decrease in arterial blood pressure when administered i.v. both as a bolus and infusion to spontaneously hypertensive rats. In contrast, no significant changes in heart rate were observed In ex vivo experiments, where porcine hearts from a slaughterhouse were used to decrease the need for laboratory animals, 3-HPAA relaxed precontracted porcine coronary artery segments via a mechanism partially dependent on endothelium integrity. This relaxation was significantly impaired after endothelial nitric oxide synthase inhibition. In contrast, the blockade of SKCa or IKCa channels, or muscarinic receptors, did not affect 3-HPAA relaxation. Similarly, no effects of 3-HPAA on cyclooxygenase nor L-type calcium channels were observed Thus, 3-HPAA decreases blood pressure in vivo via vessel relaxation, and this mechanism might be based on the release of nitric oxide by the endothelial layer. The experimental process involved the reaction of 3-Hydroxyphenylacetic acid(cas: 621-37-4).Category: alcohols-buliding-blocks

The Article related to blood pressure flavonoid metabolite 3hydroxyphenylacetic acid, 3-hydroxyphenylacetic acid, artery, blood pressure, coronary, flavonoids, gut microbiota, metabolite, pig, rat, vasorelaxation and other aspects.Category: alcohols-buliding-blocks

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Alcohol – Wikipedia,
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