Month: November 2022

On April 22, 2021, Kuehl, Nikos; Leuthold, Mila M.; Behnam, Mira A. M.; Klein, Christian D. published an article.Category: alcohols-buliding-blocks The title of the article was Beyond Basicity: Discovery of Nonbasic DENV-2 Protease Inhibitors with Potent Activity in Cell Culture. And the article contained the following:

The viral serine protease NS2B-NS3 is one of the promising targets for drug discovery against dengue virus and other flaviviruses. The mol. recognition preferences of the protease favor basic, pos. charged moieties as substrates and inhibitors, which leads to pharmacokinetic liabilities and off-target interactions with host proteases such as thrombin. We here present the results of efforts that were aimed specifically at the discovery and development of noncharged, small-mol. inhibitors of the flaviviral proteases. A key factor in the discovery of these compounds was a cellular reporter gene assay for the dengue protease, the DENV2proHeLa system. Extensive structure-activity relationship explorations resulted in novel benzamide derivatives with submicromolar activities in viral replication assays (EC50 0.24μM), selectivity against off-target proteases, and negligible cytotoxicity. This structural class has increased drug-likeness compared to most of the previously published active-site-directed flaviviral protease inhibitors and includes promising candidates for further preclin. development. The experimental process involved the reaction of H-Phg(4-OH)-OH(cas: 32462-30-9).Category: alcohols-buliding-blocks

The Article related to nonbasic small mol denv2 protease inhibitor, denv2 inhibitor structure activity relationship antiviral agent, General Organic Chemistry: Synthetic Methods and other aspects.Category: alcohols-buliding-blocks

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On August 31, 2022, Sun, Min-Fei; Xu, Youfu; Yuan, Jun-Jie; Fang, Wei-Jie published an article.COA of Formula: C3H6O4 The title of the article was Identification and characterization of chemical and physical stability of insulin formulations utilizing degraded glycerol after repeated use and storage. And the article contained the following:

Insulin treatment is currently considered to be the main strategy for controlling diabetes. Although the recombinant insulin formulation is relatively mature, we found that a batch of insulin formulation exhibited an unusual degradation rate in the stability experiment The main purposes of this article are to identify the root cause for this phenomenon and characterize of chem. and phys. degradation products. We compared the chem. and phys. stability of two batches of insulin formulations prepared sep. with simulated repeated use and freshly opened glycerol. The chem. stability of insulin was identified by liquid chromatog. coupled with tandem mass spectrometry (LC- MS/MS). Micro-flow imaging (MFI), far-UV CD (Far-UV CD) and Thioflavin T (ThT) fluorescent assays were used to reveal protein aggregation and fibrosis. The chem. and phys. stability of the insulin formulation with newly opened glycerol was much better than that with degraded glycerol, and both groups of formulations were extremely sensitive to light. The results indicated that the original batch insulin formulation with abnormal stability was indeed caused by the excipient glycerol after long-term storage and repeated usage. More attention should be paid to the quality changes of excipients during repeated usage and storage of excipients for the practical purpose. Moreover, we have discovered a novel degradation pathway for insulin and peptides in general. In addition, LC-MS/MS results suggested that the N-terminus of insulin B-chain was prone to chem. degradation which enlightens that it could be potentially modified to improve the stability of insulin formulations. The experimental process involved the reaction of 2,3-Dihydroxypropanoic acid(cas: 473-81-4).COA of Formula: C3H6O4

The Article related to chem phys stability insulin formulation glycerol, formulation, glycerol, insulin, lc-ms/ms, stability, stress test, sub-visible particle, Pharmaceuticals: Formulation and Compounding and other aspects.COA of Formula: C3H6O4

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Li, Yuehui; Topf, Christoph; Cui, Xinjiang; Junge, Kathrin; Beller, Matthias published an article in 2015, the title of the article was Lewis Acid Promoted Ruthenium(II)-Catalyzed Etherifications by Selective Hydrogenation of Carboxylic Acids/Esters.Recommanded Product: Isochroman-3-ol And the article contains the following content:

Ethers are of fundamental importance in organic chem. and they are an integral part of valuable flavors, fragrances, and numerous bioactive compounds In general, the reduction of esters constitutes the most straightforward preparation of ethers. Unfortunately, this transformation requires large amounts of metal hydrides. Presented herein is a bifunctional catalyst system, consisting of Ru/phosphine complex and aluminum triflate, which allows selective synthesis of ethers by hydrogenation of esters or carboxylic acids. Different lactones were reduced in good yields to the desired products. Even challenging aromatic and aliphatic esters were reduced to the desired products. Notably, the in situ formed catalyst can be reused several times without any significant loss of activity. The experimental process involved the reaction of Isochroman-3-ol(cas: 42900-89-0).Recommanded Product: Isochroman-3-ol

The Article related to lewis acid ruthenium catalyst etherification hydrogenation carboxylate ester, lewis acids, ethers, homogeneous catalysis, hydrogenation, ruthenium, General Organic Chemistry: Synthetic Methods and other aspects.Recommanded Product: Isochroman-3-ol

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On December 25, 1991, Nakada, Masanori; Inoue, Shintaro; Tonomura, Mikio published a patent.Computed Properties of 62640-03-3 The title of the patent was Ethanolamine derivatives for treatment of diseases accompanied by excessive collagen accumulation. And the patent contained the following:

R1NR2CHR3CH2OH (R1, R2 = H, Me; R3 = H, Me, Et; R1 = R2 = R3 ≠ H) or their pharmacol. acceptable salts are useful for treatment of diseases, such as hepatic fibrosis (including cirrhosis and chronic hepatitis), pulmonary fibrosis, keloid, scleroderma, etc. An aqueous 600 μM N-methylethanolamine (I) solution (2 mL) was added to a 2 mL a medium containing human HT-P11 fibrosarcoma cells to show 224% promotion of procollagenase production by the cells. Rats with hepatic fibrosis were administered p.o. with an aqueous 66.6 mg I/mL solution at 3 mL/kg/day for 7 wk to show serum levels of glutamic-pyruvic transaminase 436, glutamic-oxaloacetic transaminase 1250, and γ-glutamyl transpeptidase 7.0 U/L, vs. 948, 2170, and 17.6 U/L, resp., for controls without administration of I. I also lowered the serum levels of total bilirubin, alk. phosphatase, thymol turbidity, and ZnSO4 turbidity. I at 2 g/kg p.o. showed no mortality in mice. Tablets (200 mg each) containing I.HCl 50, lactose 10, corn starch 30, crystalline cellulose 8, hydroxypropyl cellulose 1, and Mg stearate 1 g were formulated. The experimental process involved the reaction of 2-(Methylamino)ethan-1-ol hydrochloride(cas: 62640-03-3).Computed Properties of 62640-03-3

The Article related to liver lung fibrosis treatment ethanolamine, cirrhosis hepatitis treatment ethanolamine, scleroderma treatment procollagenase production ethanolamine, Pharmaceuticals: Formulation and Compounding and other aspects.Computed Properties of 62640-03-3

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On June 30, 2006, Fekete, Agnes; Hertkorn, Norbert; Frommberger, Moritz; Lahaniatis, Majlinda R.; Kettrup, Antonius; Schmitt-Kopplin, Philippe published an article.SDS of cas: 4719-04-4 The title of the article was Development of a capillary electrophoresis-mass spectrometry method for the determination of formaldehyde releasers as their hydrolysis products and amino alcohols from metal working fluids. And the article contained the following:

Metal working fluids (MWFs) are widely used as lubricants and coolants for different industrial operations. Biocides are ingredients of MWFs to control the microbial growth; derivatives of hexahydrotriazines and oxazolidines are generally used. Because of the lack of appropriate characterization, an existing capillary electrophoretic method for their quantification was improved. During the process of optimization, it became clear that hydrolysis products, derivatives of amino alcs., severely interfere with the separation procedure. Since indirect-UV detection lacked the required selectivity, mass-selective detection was employed. NMR and MS established the absence of amino alcs. in the original products. The aqueous solutions of the biocides stored for extended time remained amino alc.-free, suggesting that these amino alcs. are formed from the biocides during the capillary electrophoretic separation The observation of narrow and sym. peaks indicated hydrolysis, and the polarity of the products implied favorable conditions for capillary electrophoretic separation Methods were optimized for the anal. of the amino alcs., the hydrolytic products of the formaldehyde releasers, using indirect-UV and MS detection. This method was extended to other likely solutes used as alk.-reserve ingredients. The analytes were separated within 9 min with a high precision of migration times (the RSDs were <1.5%). When quantifying from mobility scale, the calibration curves produced linearity with regression coefficients at 0.990-0.999. The detection limit was <1 mg/L in the case of MS detection. The influence of water-based MWF was also studied, and no matrix effect on the migration of the analytes and on the peak areas was observed The experimental process involved the reaction of 2,2',2''-(1,3,5-Triazinane-1,3,5-triyl)triethanol(cas: 4719-04-4).SDS of cas: 4719-04-4

The Article related to metal working fluid biocide hydrolytic product analysis electrophoresis ms, capillary electrophoresis mass spectrometry amino alc metal working fluid, Organic Analytical Chemistry: Determinations and other aspects.SDS of cas: 4719-04-4

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On June 30, 2021, Lagerspets, Emi; Valbonetti, Evelyn; Eronen, Aleksi; Repo, Timo published an article.Recommanded Product: 111-29-5 The title of the article was A new catalytic approach for aerobic oxidation of primary alcohols based on a Copper(I)-thiophene carbaldimines. And the article contained the following:

Novel Cu(I) thiophene carbaldimine catalysts for the selective aerobic oxidation of primary alcs. to their corresponding aldehydes and various diols to lactones or lactols was reported. In the presence of the in-situ generated Cu(I) species, a persistent radical (2,2,6,6-tetramethylpiperdine-N-oxyl (TEMPO)) and N-methylimidazole (NMI) as an auxiliary ligand, the reaction proceeds under aerobic conditions and at ambient temperature Especially the catalytic system of 1-(thiophen-2-yl)-N-(4-(trifluoromethoxy)phenyl)methanimine with copper(I)-iodide showed high reactivity for all kind of alcs. (benzylic, allylic and aliphatic). In the case of benzyl alc. even 2.5 mol% of copper loading gave quant. yield. Beside high activity under aerobic conditions, the catalysts ability to oxidize 1,5-pentadiol to the corresponding lactol (86% in 4 h) and N-phenyldiethanolamine to the corresponding morpholine derivate lactol (86% in 24 h) is particularly noteworthy. The experimental process involved the reaction of Pentane-1,5-diol(cas: 111-29-5).Recommanded Product: 111-29-5

The Article related to thiophenyl methanimine preparation, primary alc copper thiophenyl methanimine catalyst oxidation, diol copper thiophenyl methanimine catalyst oxidation, General Organic Chemistry: Synthetic Methods and other aspects.Recommanded Product: 111-29-5

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On September 30, 2021, Nishad, Jay Hind; Singh, Arti; Gautam, Veer Singh; Kumari, Puja; Kumar, Jitendra; Yadav, Monika; Kharwar, Ravindra Nath published an article.Recommanded Product: 2,4-Di-tert-butylphenol The title of the article was Bioactive potential evaluation and purification of compounds from an endophytic fungus Diaporthe longicolla, a resident of Saraca asoca (Roxb.) Willd.. And the article contained the following:

An endophytic fungus (L3), isolated from the leaf tissues of Saraca asoca was identified as D. longicolla by microscopic and mol. methods. The crude extracts of D. longicolla revealed to harbor seven compounds in GC-MS anal. which was subjected to a thin layer chromatog. (TLC) for purification and separation of bioactive ingredients. The partially purified fraction from TLC displayed the presence of 2-tridecene (Z) (RT-14.50), 5-tridecene (E) (RT-16.65) and 2,4-di-tert-butylphenol (RT-13.92) in GC-MS. High-performance liquid chromatog. (HPLC) was performed to further purify the constituents which led to the collection of 2,4-di-tert-Bu phenol (RT-2.34) with excellent antioxidant activity and antibacterial activity against methicillin resistance Staphylococcus aureus (MRSA). The experimental process involved the reaction of 2,4-Di-tert-butylphenol(cas: 96-76-4).Recommanded Product: 2,4-Di-tert-butylphenol

The Article related to saraca asoca diaporthe longicolla resident compound purification bioactivity, bioactivity evaluation, compound purification, d. longicolla, gc–ms, hplc, Plant Biochemistry: Composition and Products and other aspects.Recommanded Product: 2,4-Di-tert-butylphenol

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On August 1, 2020, Toyooka, Genki; Fujita, Ken-ichi published an article.Quality Control of Pentane-1,5-diol The title of the article was Synthesis of Dicarboxylic Acids from Aqueous Solutions of Diols with Hydrogen Evolution Catalyzed by an Iridium Complex. And the article contained the following:

A catalytic system for the synthesis of dicarboxylic acids e.g., glutaric acid from aqueous solutions of diols e.g., pentane-1,5-diol accompanied by the evolution of hydrogen was developed. An iridium complex bearing a functional bipyridonate ligand with N,N-dimethylamino substituents exhibited a high catalytic performance for this type of dehydrogenative reaction. For example, adipic acid was synthesized from an aqueous solution of 1,6-hexanediol in 97% yield accompanied by the evolution of four equivalent of hydrogen by the present catalytic system. It should be noted that the simultaneous production of industrially important dicarboxylic acids and hydrogen, which is useful as an energy carrier, was achieved. In addition, the selective dehydrogenative oxidation of vicinal diols CH3(CH2)nCH(OH)CH2OH (n = 0, 1, 2, 3) to give α-hydroxycarboxylic acids CH3(CH2)nCH(OH)COOH was also accomplished. The experimental process involved the reaction of Pentane-1,5-diol(cas: 111-29-5).Quality Control of Pentane-1,5-diol

The Article related to dicarboxylic acid preparation, diol hydrogen evolution iridium catalyst, dehydrogenation, dicarboxylic acids, diols, iridium, α-hydroxycarboxylic acids, General Organic Chemistry: Synthetic Methods and other aspects.Quality Control of Pentane-1,5-diol

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On April 21, 2021, Sun, Xiangshi; Yu, Kongtong; Zhou, Yulin; Dong, Shiyan; Hu, Wenji; Sun, Yating; Li, Yuhuan; Xie, Jing; Lee, Robert J.; Sun, Fengying; Ma, Yifan; Wang, Shengnian; Kim, Betty Y. S.; Wang, Yifan; Yang, Zhaogang; Jiang, Wen; Li, Youxin; Teng, Lesheng published an article.Category: alcohols-buliding-blocks The title of the article was Self-Assembled pH-Sensitive Polymeric Nanoparticles for the Inflammation-Targeted Delivery of Cu/Zn-Superoxide Dismutase. And the article contained the following:

The use of superoxide dismutase (SOD) is currently limited by its short half-life, rapid plasma clearance rate, and instability. We synthesized a small library of biofriendly amphiphilic polymers that comprise methoxy poly(ethylene glycol)-poly(cyclohexane-1,4-diyl acetone dimethyleneketal) (mPEG-PCADK) and mPEG-poly((cyclohexane86.7%, 1,5-pentanediol13.3%)-1,4-diyl acetone dimethylene ketal) (PK3) for the targeted delivery of SOD. The novel polymers could self-assemble into micellar nanoparticles with favorable hydrolysis kinetics, biocompatibility, long circulation time, and inflammation-targeting effects. These materials generated a better pH-response curve and exhibited better hydrolytic kinetic behavior than PCADK and PK3. The polymers showed good biocompatibility with protein drugs and did not induce an acidic microenvironment during degradation in contrast to materials such as PEG-block-poly(lactic-co-glycolic acid) (PLGA) and PLGA. The SOD that contained reverse micelles based on mPEG2000-PCADK exhibited good circulation and inflammation-targeting properties. Pharmacodynamic results indicated exceptional antioxidant and anti-inflammatory activities in a rat adjuvant-induced arthritis model and a rat peritonitis model. These results suggest that these copolymers are ideal protein carriers for targeting inflammation treatment. The experimental process involved the reaction of Pentane-1,5-diol(cas: 111-29-5).Category: alcohols-buliding-blocks

The Article related to polyketal ph sensitive nanoparticle copper zinc superoxide dismutase, cu/zn-superoxide dismutase, drug delivery, nanoparticles, ph-sensitive, polyketals, Pharmaceuticals: Formulation and Compounding and other aspects.Category: alcohols-buliding-blocks

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Kowalski, Piotr S.; Capasso Palmiero, Umberto; Huang, Yuxuan; Rudra, Arnab; Langer, Robert; Anderson, Daniel G. published an article in 2018, the title of the article was Ionizable amino-polyesters synthesized via ring opening polymerization of tertiary amino-alcohols for tissue selective mRNA delivery.Electric Literature of 4719-04-4 And the article contains the following content:

The utility of mRNA (mRNA) as a therapy is gaining a broad interest due to its potential for addressing a wide range of diseases, while effective delivery of mRNA mols. to various tissues still poses a challenge. This study reports on the design and characterization of new ionizable amino-polyesters (APEs), synthesized via ring opening polymerization (ROP) of lactones with tertiary amino-alcs. that enable tissue and cell type selective delivery of mRNA. With a diverse library of APEs formulated into lipid nanoparticles (LNP), structure-activity parameters crucial for efficient transfection are established and APE-LNPs are identified that can preferentially home to and elicit effective mRNA expression with low in vivo toxicity in lung endothelium, liver hepatocytes, and splenic antigen presenting cells, including APE-LNP demonstrating nearly tenfold more potent systemic mRNA delivery to the lungs than vivo-jetPEI. Adopting tertiary amino-alcs. to initiate ROP of lactones allows to control polymer mol. weight and obtain amino-polyesters with narrow mol. weight distribution, exhibiting batch-to-batch consistency. All of which highlight the potential for clin. translation of APEs for systemic mRNA delivery and demonstrate the importance of employing controlled polymerization in the design of new polymeric nanomaterials to improve in vivo nucleic acid delivery. The experimental process involved the reaction of 2,2′,2”-(1,3,5-Triazinane-1,3,5-triyl)triethanol(cas: 4719-04-4).Electric Literature of 4719-04-4

The Article related to aminopolyester synthesis tertiary amino alc mrna delivery tissue, biomaterials, messenger rna, nucleic acid delivery, polyesters, polymeric nanoparticles, Pharmaceuticals: Formulation and Compounding and other aspects.Electric Literature of 4719-04-4

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