Author: tianli

Qiu, Qianqian published the artcileDesign, synthesis, and biological evaluation of novel FXR agonists based on auraptene, Related Products of alcohols-buliding-blocks, the publication is Bioorganic Chemistry (2021), 105198, database is CAplus and MEDLINE.

Farnesoid X receptor (FXR) has been considered as an attractive target for metabolic disorder and liver injury, while many current FXR agonists suffer from undesirable side effects, such as pruritus. Therefore, it is urgent to develop new structure types different from current FXR agonists. In this study, a series of structural optimizations were introduced to displace the unstable coumarin and geraniol scaffolds of auraptene (AUR), a novel and safe FXR agonist. All of these efforts led to the identification of compound 14 (I), a potent FXR agonist with nearly fourfold higher activity than AUR. Mol. modeling study suggested that compound 14 fitted well with binding pocket, and formed the key ionic bond with His291 and Arg328. In acetaminophen-induced acute liver injury model, compound 14 exerts better therapeutic effect than that of AUR, which highlighting its pharmacol. potential in the treatment of drug-induced liver injury.

Bioorganic Chemistry published new progress about 621-37-4. 621-37-4 belongs to alcohols-buliding-blocks, auxiliary class Carboxylic acid,Benzene,Phenol,Natural product, name is 3-Hydroxyphenylacetic acid, and the molecular formula is C8H8O3, Related Products of alcohols-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Shang, Yong-Jia published the artcileSoluble polymer-supported synthesis of isoxazoles, Product Details of C10H8ClNO2, the publication is Tetrahedron Letters (2002), 43(12), 2247-2249, database is CAplus.

The first soluble polymer-supported synthesis of isoxazoles through a 1,3-dipolar cycloaddition is described. A soluble polymer-supported alkyne reacts with nitrile oxides generated in situ to give isoxazoles in good yield.

Tetrahedron Letters published new progress about 438565-33-4. 438565-33-4 belongs to alcohols-buliding-blocks, auxiliary class Isoxazole,Chloride,Benzene,Alcohol, name is 3-(2-Chlorophenyl)-5-isoxazolemethanol, and the molecular formula is C10H10O2, Product Details of C10H8ClNO2.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Shang, Yong-Jia published the artcileSynthesis of isoxazolines and isoxazoles using poly(ethylene glycol) as support, Product Details of C10H8ClNO2, the publication is Synthesis (2002), 1663-1668, database is CAplus.

A general method for the liquid-phase syntheses of isoxazoles and isoxazolines through a 1,3-dipolar cycloaddition is described. The poly(ethylene glycol) (PEG)-supported alkyne or alkene reacted with nitrile oxides generated in situ from aldoximes, followed by cleavage from the PEG, to give isoxazoles or isoxazolines in good yield and purity.

Synthesis published new progress about 438565-33-4. 438565-33-4 belongs to alcohols-buliding-blocks, auxiliary class Isoxazole,Chloride,Benzene,Alcohol, name is 3-(2-Chlorophenyl)-5-isoxazolemethanol, and the molecular formula is C4H3Cl2N3, Product Details of C10H8ClNO2.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Shi, Jinguo published the artcileSynthesis and biological evaluation of 1,2,4-oxadiazole core derivatives as potential neuroprotectants against acute ischemic stroke, Category: alcohols-buliding-blocks, the publication is Neurochemistry International (2021), 105103, database is CAplus and MEDLINE.

Here, we report the synthesis and neuroprotective capacity of 27 compounds with a bisphenol hydroxyl-substituted 1,2,4-triazole core or 1,2,4-oxadiazole core for stroke therapy. In vitro studies of the neuroprotective effects of compounds 1-27 on sodium nitroprusside (SNP)-induced apoptosis in PC12 cells indicate that compound 24 is the most effective compound conferring potent protection against oxidative injury. Compound 24 inhibits reactive oxygen species (ROS) accumulation and restores the mitochondrial membrane potential (MMP). Moreover, further anal. of the mechanism showed that compound 24 activates the antioxidant defense system by promoting the nuclear translocation of nuclear factor erythroid 2-related factor 2 (Nrf2) and increasing the expression of haem oxygenase 1 (HO-1). An in vivo study was performed in a rat model of transient focal cerebral ischemia generated by the intraluminal occlusion of the middle cerebral artery (MCAO). Compound 24 significantly reduced brain infarction and improved neurol. function. Overall, compound 24 potentially represents a promising compound for the treatment of stroke.

Neurochemistry International published new progress about 328-90-5. 328-90-5 belongs to alcohols-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Carboxylic acid,Benzene,Phenol, name is 2-Hydroxy-4-(trifluoromethyl)benzoic acid, and the molecular formula is C12H13F2N3O4S, Category: alcohols-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Bai, Xinxin published the artcileRemediation of phenanthrene contaminated soil by coupling soil washing with Tween 80, oxidation using the UV/S₂O₈^2- process and recycling of the surfactant, Application of 1-Hydroxy-2-naphthoic acid, the publication is Chemical Engineering Journal (Amsterdam, Netherlands) (2019), 1014-1023, database is CAplus.

Surfactant-enhanced soil washing was applied to phenanthrene (PHE)-polluted soil, followed by a sulfate radical-based advanced oxidation process. Soil washing experiments were conducted using the nonionic surfactant Tween 80 (TW 80), assessing the effect of washing temperature, TW 80 concentration, and liquid:soil ratio on PHE removal. Maximum PHE removal (90.0%) was achieved with 15 g/L TW 80 and a 10:1 (mL/g) liquid:soil ratio at 20°. A UV/S₂O₈^2- process was used to selectively oxidize PHE in the effluent and recover TW 80. The regenerated effluent was re-used for soil washing; results showed PHE removal efficiency was nearly the same as with fresh surfactant solution The UV/S₂O₈^2- oxidation reaction was also assessed, including possible intermediate products detection by liquid chromatog./mass spectrometry; a corresponding degradative pathway of target pollutants was proposed. Overall result indicated toil washing with TW 80 and subsequent selective UV/S₂O₈^2- oxidation may provide a potential option to remediate polycyclic aromatic hydrocarbon-polluted soil.

Chemical Engineering Journal (Amsterdam, Netherlands) published new progress about 86-48-6. 86-48-6 belongs to alcohols-buliding-blocks, auxiliary class Organic Pigment,Natural product, name is 1-Hydroxy-2-naphthoic acid, and the molecular formula is C11H8O3, Application of 1-Hydroxy-2-naphthoic acid.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Liu, Yan published the artcileBiocatalytic synthesis of C3 chiral building blocks by chloroperoxidase-catalyzed enantioselective halo-hydroxylation and epoxidation in the presence of ionic liquids, Application of (R)-Oxiran-2-ylmethanol, the publication is Biotechnology Progress (2015), 31(3), 724-729, database is CAplus and MEDLINE.

The optically active C3 synthetic blocks are remarkably versatile intermediates for the synthesis of numerous pharmaceuticals and agrochems. This work provides a simple and efficient enzymic synthetic route for the environment-friendly synthesis of C3 chiral building blocks. Chloroperoxidase (CPO)-catalyzed enantioselective halo-hydroxylation and epoxidation of chloropropene and allyl alc. was employed to prepare C3 chiral building blocks in this work, including (R)-2,3-dichloro-1-propanol (DCP*), (R)-2,3-epoxy-1-propanol (GLD*), and (R)-3-chloro-1-2-propanediol (CPD*). The ee values of the formed C3 chiral building blocks DCP*, CPD*, and glycidol were 98.1, 97.5, and 96.7%, resp. Moreover, the use of small amount of imidazolium ionic liquid enhanced the yield efficiently due to the increase of solubility of hydrophobic organic substrates in aqueous reaction media, as well as the improvement of affinity and selectivity of CPO to substrate. © 2015 American Institute of Chem. Engineers Biotechnol. Prog., 2015.

Biotechnology Progress published new progress about 57044-25-4. 57044-25-4 belongs to alcohols-buliding-blocks, auxiliary class Epoxides,Chiral,Aliphatic hydrocarbon chain,Alcohol, name is (R)-Oxiran-2-ylmethanol, and the molecular formula is C3H6O2, Application of (R)-Oxiran-2-ylmethanol.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Zhang, Yajie published the artcileTargeted Gene Delivery to Macrophages by Biodegradable Star-Shaped Polymers, Quality Control of 96345-79-8, the publication is ACS Applied Materials & Interfaces (2016), 8(6), 3719-3724, database is CAplus and MEDLINE.

In this report, two biodegradable star-shaped polyasparamide derivatives and four analogs modified with either mannose or folic acid moiety for preferential targeting of a difficult-to-transfect immune cell type, i.e., macrophage, have been synthesized. Each of the prepared star polymers complexes with plasmid DNA to form nanosized particles featuring a core-shell-like morphol. Mannose or folate functionalized star polymers can greatly improve the transfection performance on a macrophage cell line RAW 264.7. As a result, a combination of targeting ligand modification and topol. structures of gene carriers is a promising strategy for immune cells-based gene therapy.

ACS Applied Materials & Interfaces published new progress about 96345-79-8. 96345-79-8 belongs to alcohols-buliding-blocks, auxiliary class Sugar Units,Gal and Man, name is (2R,3S,4S,5S,6R)-2-(Hydroxymethyl)-6-(4-isothiocyanatophenoxy)tetrahydro-2H-pyran-3,4,5-triol, and the molecular formula is C8H7ClO3, Quality Control of 96345-79-8.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Zhao, C. published the artcileRemoval of bisphenol S from drinking water by adsorption using activated carbon and the mechanisms involved, Quality Control of 80-09-1, the publication is International Journal of Environmental Science and Technology (2022), 19(6), 5289-5300, database is CAplus.

Bisphenol S, an alternative chem. to bisphenol A, has a neg. effect on living organisms and has frequently been detected in drinking water systems. A promising and cost-effective method for removing bisphenol S from tap water is adsorption by activated carbon. However, activated carbon significantly decreased the adsorption capacity of bisphenol S in tap water comparing with that in deionized water based on the exptl. results. Dissolved organic matter in tap water was likely responsible for it. The adsorption kinetics can be described by a pseudo-second-order model. The Langmuir isotherm model can well describe the process, suggesting monolayer adsorption. The maximum adsorption capacity was calculated as 83.19 mg g^-1. Higher temperature and pH were unfavorable to the process. Changes in entropy, enthalpy, and Gibbs free energy were calculated and implied a spontaneous and exothermic adsorption process. Fourier transform IR spectroscopic anal. found that hydroxyl and amino functional groups are the main groups involved. The research provides a substantial basis for understanding bisphenol S removal from drinking water by adsorption using activated carbon to limit direct exposure to bisphenol S in drinking water.

International Journal of Environmental Science and Technology published new progress about 80-09-1. 80-09-1 belongs to alcohols-buliding-blocks, auxiliary class Ploymers, name is 4,4′-Sulfonyldiphenol, and the molecular formula is C18H23OP, Quality Control of 80-09-1.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Zhang, Xue-Qing published the artcileGalactosylated ternary DNA/polyphosphoramidate nanoparticles mediate high gene transfection efficiency in hepatocytes, Related Products of alcohols-buliding-blocks, the publication is Journal of Controlled Release (2005), 102(3), 749-763, database is CAplus and MEDLINE.

Galactosylated polyphosphoramidates (Gal-PPAs) with different ligand substitution degrees (6.5%, 12.5% and 21.8%, resp.) were synthesized and evaluated as hepatocyte-targeted gene carriers. The in vitro cytotoxicity of Gal-PPA decreased significantly with an increase in galactose substitution degree. The affinity of Gal-PPA/DNA nanoparticles to galactose-recognizing lectin increased with galactose substitution degree. However, decreased transfection efficiency was observed for these galactosylated PPAs in HepG2 cells. Based on the results of gel retardation and polyanion competition assays, we hypothesized that the reduced transfection efficiency of Gal-PPA/DNA nanoparticles was due to their decreased DNA-binding capacity and decreased particle stability. We therefore prepared nanoparticles by precondensing DNA with PPA at a charge ratio of 0.5, yielding nanoparticles with neg. surface charge, followed by coating with Gal-PPA, resulting in a Gal-PPA/ DNA/PPA ternary complex. Such a ternary nanoparticle formulation led to significant size reduction in comparison with binary nanoparticles, particularly at low N/P ratios (2 to 5). In HepG2 cells and primary rat hepatocytes, and at low N/P ratios (2 to 5), transfection efficiency mediated by ternary nanoparticles prepared with 6.5% Gal-PPA was 6-7200 times higher than PPA-DPA/DNA nanoparticles. Transgene expression increased slightly at higher N/P ratios in HepG2 cells and reached a plateau at N/P ratios between 5 and 10 for primary rat hepatocytes. Such an enhancement effect was not observed in HeLa cells that lack of asialoglycoprotein receptor (ASGPR). Nevertheless, transfection efficiency of ternary particles decreased dramatically, presumably due to the decreased DNA binding capacity and particle stability, as PPA galactosylation degree increased. This highlights the importance of optimizing ligand conjugation degree for PPA gene carrier.

Journal of Controlled Release published new progress about 96345-79-8. 96345-79-8 belongs to alcohols-buliding-blocks, auxiliary class Sugar Units,Gal and Man, name is (2R,3S,4S,5S,6R)-2-(Hydroxymethyl)-6-(4-isothiocyanatophenoxy)tetrahydro-2H-pyran-3,4,5-triol, and the molecular formula is C10H10CoF6P, Related Products of alcohols-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Zhang, Jun published the artcile(E)-β-Trifluoromethyl vinylsulfones as antitumor agents: Synthesis and biological evaluations, Category: alcohols-buliding-blocks, the publication is European Journal of Medicinal Chemistry (2022), 114197, database is CAplus and MEDLINE.

A three-component reaction of phenylacetylene, trifluoromethyl thianthrenium triflate (TT-CF+3OTf-) and sodium sulfinates under extremely mild conditions is developed, leading to various trifluoromethyl-substituted vinyl sulfones in moderate to good yields with excellent stereoselectivity. Addnl., elaboration of trifluoromethyl-substituted vinyl sulfone by palladium-catalyzed amination is performed. These trifluoromethyl-substituted vinyl sulfones are further evaluated for several assays against different tumor cells and the antitumor mechanism in cytotoxic autophagy induced by PI3K/Akt/mTOR signal is investigated.

European Journal of Medicinal Chemistry published new progress about 622-40-2. 622-40-2 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Alcohol, name is 2-Morpholinoethanol, and the molecular formula is C9H9NO6S, Category: alcohols-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts