Tag: 100-200

On October 31, 2022, Liu, Siyao; Fang, Zhongxiang; Ng, Ken published an article.HPLC of Formula: 621-37-4 The title of the article was Incorporating inulin and chitosan in alginate-based microspheres for targeted delivery and release of quercetin to colon. And the article contained the following:

Colon targeted delivery of quercetin by encapsulation has the potential to manage colonic diseases due to quercetin’s pharmacol. effects. To strengthen the functionalities of commonly used alginate microspheres for quercetin encapsulation, inulin was added as filling material and chitosan as coating material. Empty/quercetin-loaded alginate (AL-E/Q), alginate + inulin (ALIN-E/Q), alginate + inulin + chitosan (ALINCH-E/Q) microspheres were fabricated, with particle sizes ranging from 25.1 ± 1.8 to 79.4 ± 4.5μm. All the formulated microspheres were neg. charged, and zeta potential was dependent mainly on chitosan coating and the pH of surrounding media. FTIR spectra of the microspheres suggested successful encapsulation of quercetin, formation of chitosan coating and potential hydrogen bonding between inulin and alginate. Scanning electron micrographs showed that inulin filling enhanced gel strength by filling up the pores in the alginate polymer network, and that loading of quercetin also helped to fill up the pores compared to empty microspheres. Combination of inulin as filling material and chitosan as coating material in quercetin loaded ALINCH-Q achieved superior performance compared to other formulations with encapsulation efficiency of 53.2 ± 1.2%, and retention rate of the loaded quercetin up to 80.3 ± 4.4% through in vitro gastrointestinal digestion, thus was chosen for colonic fermentation Subjecting ALINCH-Q to colonic fermentation using pig fecal material as microbiota source showed that quercetin release was delayed but occurred within 3 h of fermentation and was completely metabolized by the microbiota by 24 h. Thus, ALINCH-Q microsphere showed potential in targeted delivery and release of quercetin to the colon. The experimental process involved the reaction of 3-Hydroxyphenylacetic acid(cas: 621-37-4).HPLC of Formula: 621-37-4

The Article related to inulin chitosan alginate quercetin microsphere drug delivery sustained release, colonic disease, encapsulation, gut microbiota, in vitro digestion, inulin, quercetin, Pharmaceuticals: Formulation and Compounding and other aspects.HPLC of Formula: 621-37-4

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On December 9, 2020, Lv, Jia; Wang, Changping; Li, Hongru; Li, Zhan; Fan, Qianqian; Zhang, Ying; Li, Yiwen; Wang, Hui; Cheng, Yiyun published an article.Computed Properties of 143-10-2 The title of the article was Bifunctional and Bioreducible Dendrimer Bearing a Fluoroalkyl Tail for Efficient Protein Delivery Both In Vitro and In Vivo. And the article contained the following:

Rational design of stimuli-responsive polymers for cytosolic protein delivery with robust efficiency is of great importance but remains a challenging task. Here, we reported a bioreducible and amphiphilic dendrimer bearing a fluoroalkyl tail for this purpose. The fluorolipid was conjugated to the focal point of a cysteamine-cored polyamidoamine dendrimer via disulfide bond, while phenylboronic acid moieties were decorated on dendrimer surface for efficient protein binding. The yielding polymer showed high protein binding capability and complex stability and could efficiently release the cargo proteins in a glutathione-responsive manner. The designed polymer was effective in the delivery of various membrane-impermeable proteins into living cells with reserved bioactivities. In addition, the polymer efficiently delivered a toxin protein saporin into 4T1 breast cancer cells and inhibited the tumor growth in vivo after i.v. injection. The developed polymer in this study is a promising vector for the delivery of membrane-impermeable proteins to treat various diseases. The experimental process involved the reaction of 1-Decanethiol(cas: 143-10-2).Computed Properties of 143-10-2

The Article related to bifunctional bioreducible dendrimer fluoroalkyl protein cytosol delivery cancer therapy, responsive polymer, cancer therapy, cytosolic protein delivery, dendrimer, Pharmaceuticals: Formulation and Compounding and other aspects.Computed Properties of 143-10-2

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

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

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

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

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

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

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

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

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

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

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

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

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

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

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On April 15, 2020, Iliopoulos, Fotis; Sil, Bruno C.; Monjur Al Hossain, A. S. M.; Moore, David J.; Lucas, Robert A.; Lane, Majella E. published an article.Synthetic Route of 111-29-5 The title of the article was Topical delivery of niacinamide: Influence of neat solvents. And the article contained the following:

Niacinamide (NIA) has been widely used in cosmetic and personal care formulations for several skin conditions. Permeation of topical NIA has been confirmed in a number of studies under infinite dose conditions. However, there is limited information in the literature regarding permeation of NIA following application of topical formulations in amounts that reflect the real-life use of such products by consumers. The aim of the present work was therefore to investigate skin delivery of NIA from single solvent systems in porcine skin under finite dose conditions. A secondary aim was to probe the processes underlying the previously reported low recovery of NIA following in vitro permeation and mass balance studies. The solubility and stability of NIA in various single solvent systems was examined The solvents investigated included Transcutol P (TC), propylene glycol (PG), 1-2 hexanediol (HEX), 1-2 pentanediol (1-2P), 1-5 pentanediol (1-5P), 1-3 butanediol (1-3B), glycerol (GLY) and di-Me isosorbide (DMI). Skin permeation and deposition of the mol. was investigated in full thickness porcine skin in vitro finite dose Franz-type diffusion experiments followed by mass balance studies. Stability of NIA for 72 h in the solvents was confirmed. The solubility of NIA in the solvents ranged from 82.9 ± 0.8 to 311.9 ± 4.5 mg/mL. TC delivered the highest percentage permeation of NIA at 24 h, 32.6 ± 12.1% of the applied dose. Low total recovery of NIA after mass balance studies was observed for some vehicles, with values ranging from 55.2 ± 12.8% to 106.3 ± 2.3%. This reflected the formation of a number of NIA degradation byproducts in the receptor phase during the permeation studies. Identification of other vehicles for synergistic enhancement of NIA skin delivery will be the subject of future work. The experimental process involved the reaction of Pentane-1,5-diol(cas: 111-29-5).Synthetic Route of 111-29-5

The Article related to skin topical formulation solvent niacinamide, finite dose, in vitro, niacinamide, permeation, porcine skin, Pharmaceuticals: Formulation and Compounding and other aspects.Synthetic Route of 111-29-5

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts