Category: alcohols-buliding-blocks

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

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, 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

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

Yin, Yue published the artcileClinical analysis of Hemabate combined with oxytocin for prevention of postpartum hemorrhage after cesarean section in high-risk parturients, Name: 2-Amino-2-(hydroxymethyl)propane-1,3-diol (Z)-7-((1R,2R,3R,5S)-3,5-dihydroxy-2-((S,E)-3-hydroxy-3-methyloct-1-en-1-yl)cyclopentyl)hept-5-enoic acid, the publication is Xiandai Zhenduan Yu Zhiliao (2017), 28(8), 1407-1408, database is CAplus.

To observe the prevention and safety effect and safety of Hemabate combined with oxytocin on postpartum hemorrhage of cesarean women with high risk factors of postpartum hemorrhage. The 240 pregnant women undergoing cesarean section with high risk factors of postpartum hemorrhage, such as uterine weakness, placenta previa, twin pregnancy, giant fetus, polyhydramnios, scarred uterus, etc., were selected as the research subjects, and they were randomly divided into observation group and 120 cases in each control group. In the control group, oxytocin 20U was injected i.v. after the fetus was delivered to prevent postpartum hemorrhage, and the observation group was combined with the control group with 250 μg deep i.m. injection of Hemabate. We observed and compared the bleeding volume and the incidence of postpartum hemorrhage and adverse reactions during cesarean section, 2h postpartum and 24h postpartum between the two groups. In the observation group, the average blood loss at 2h and 24h after delivery was significantly lower than that in the control group (P < 0.05). The incidence of postpartum hemorrhage in the observation group was 1.67% significantly lower than 11.67% in the control group (P < 0.05). There were 16 cases of postpartum adverse reactions in the observation group, the symptoms were mild and alleviated spontaneously. For pregnant women undergoing cesarean section with high risk factors for postpartum hemorrhage. The preventive use of Hemabate significantly reduces the amount of intraoperative and postpartum hemorrhage, reduces the incidence of postpartum hemorrhage, and the medication is safe, convenient and effective.

Xiandai Zhenduan Yu Zhiliao published new progress about 58551-69-2. 58551-69-2 belongs to alcohols-buliding-blocks, auxiliary class Chiral,Alkenyl,Amine,Aliphatic cyclic hydrocarbon,Ester,Alcohol,Inhibitor,, name is 2-Amino-2-(hydroxymethyl)propane-1,3-diol (Z)-7-((1R,2R,3R,5S)-3,5-dihydroxy-2-((S,E)-3-hydroxy-3-methyloct-1-en-1-yl)cyclopentyl)hept-5-enoic acid, and the molecular formula is C10H10CoF6P, Name: 2-Amino-2-(hydroxymethyl)propane-1,3-diol (Z)-7-((1R,2R,3R,5S)-3,5-dihydroxy-2-((S,E)-3-hydroxy-3-methyloct-1-en-1-yl)cyclopentyl)hept-5-enoic acid.

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

Ge, Jie published the artcileApplication of an LC-MS/MS Method to a Urinary Excretion Study of Triflusal and its Main Metabolite 2-hydroxy-4-trifluoromethyl Benzoic Acid in Human Urine, Application of 2-Hydroxy-4-(trifluoromethyl)benzoic acid, the publication is Current Pharmaceutical Analysis (2020), 16(3), 328-334, database is CAplus.

Objective: A validated liquid chromatog.-tandem mass spectrometry method (LCMS/ MS) was established to simultaneously determine the concentration of triflusal and its main metabolite 2-hydroxy-4-trifluoromethyl benzoic acid(HTB) in human urine. Methods: The separation was performed on a Dikma C18 column using isocratic elution with acetonitrile-4 mmol/L ammonium acetate aqueous solution containing 0.3% formic acid water (78: 28, V/V). The method involved extraction with methanol using protein precipitation The precursor-to product ion transitions with multiple reaction monitoring was m/z 247.1→161.1, 204.8→106.7and 136.9→93.0 for triflusal, HTB and salicylic acid(IS), resp. The method showed good linear relationships over the ranges of 0.08 to 48μg/mL and 0.5 to 50μg/mL. Results: It was the first time that a urinary excretion study of triflusal capsule as oral. The cumulative urinary recovery showed 8.5% and 2.7% for triflusal and HTB, resp. Conclusion: This method was successfully used for evaluating the pharmacokinetic properties of triflusal and HTB in urine in Chinese healthy subjects.

Current Pharmaceutical Analysis 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 C8H5F3O3, Application of 2-Hydroxy-4-(trifluoromethyl)benzoic acid.

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

Xu, Xi published the artcileStructure-Enabled Discovery of Novel Macrocyclic Inhibitors Targeting Glutaminase 1 Allosteric Binding Site, SDS of cas: 621-37-4, the publication is Journal of Medicinal Chemistry (2021), 64(8), 4588-4611, database is CAplus and MEDLINE.

The inhibition of glutaminase 1 (GLS1) represents a potential treatment of malignant tumors. Structural anal. led to the design of a novel series of macrocyclic GLS1 allosteric inhibitors. Through extensive structure-activity relationship studies, a promising candidate mol. 13b (LL202) was identified with robust GLS1 inhibitory activity (IC₅₀ = 6 nM) and high GLS1 binding affinity (SPR, K_d = 24 nM; ITC, K_d = 37 nM). The X-ray crystal structure of the 13b-GLS1 complex was resolved, revealing a unique binding mode and providing a novel structural scaffold for GLS1 allosteric inhibitors. Importantly, 13b clearly adjusted the cellular metabolites and induced an increase in the ROS level by blocking glutamine metabolism Furthermore, 13b exhibited a similar in vivo antitumor activity as CB839. This study adds to the growing body of evidence that macrocyclization provides an alternative and complementary approach for the design of small-mol. inhibitors, with the potential to improve the binding affinity to the targets.

Journal of Medicinal 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 C20H17FO4S, SDS of cas: 621-37-4.

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

Obst, Jon K. published the artcileRevealing Metabolic Liabilities of Ralaniten To Enhance Novel Androgen Receptor Targeted Therapies, Safety of (R)-Oxiran-2-ylmethanol, the publication is ACS Pharmacology & Translational Science (2019), 2(6), 453-467, database is CAplus and MEDLINE.

Inhibition of the androgen receptor (AR) is the mainstay treatment for advanced prostate cancer. Ralaniten (formally EPI-002) prevents AR transcriptional activity by binding to its N-terminal domain (NTD) which is essential for transcriptional activity. Ralaniten acetate (EPI-506) the triacetate pro-drug of ralaniten, remains the only AR-NTD inhibitor to have entered clin. trials (NCT02606123). While well tolerated, the trial was ultimately terminated due to poor pharmacokinetic properties and resulting pill burden. Here we discovered that ralaniten was glucuronidated which resulted in decreased potency. Long-term treatment of prostate cancer cells with ralaniten results in upregulation of UGT2B enzymes with concomitant loss of potency. This has proven to be a useful model with which to facilitate the development of more potent second-generation AR-NTD inhibitors. Glucuronidated metabolites of ralaniten were also detected in the serum of patients in Phase 1 clin. trials. Therefore, we tested an analog of ralaniten (EPI-045) which was resistant to glucuronidation and demonstrated superiority to ralaniten in our resistant model. These data support that analogs of ralaniten designed to mitigate glucuronidation may optimize clin. responses to AR-NTD inhibitors.

ACS Pharmacology & Translational Science 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, Safety of (R)-Oxiran-2-ylmethanol.

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

Xia, Ziming published the artcileCopper-catalyzed domino intramolecular cyclization: a facile and efficient approach to polycyclic indole derivatives, Formula: C8H5F3O3, the publication is Organic & Biomolecular Chemistry (2012), 10(8), 1602-1611, database is CAplus and MEDLINE.

A mild and efficient Cu₂O-catalyzed domino intramol. C-N coupling/C-Y (Y = O, S, N) bond formation was successfully achieved. Thus oxazino[3,2-a]indole, thiazino[3,2-a]indole and indolo[2,1-b]quinazoline derivatives were facilely assembled from readily accessible gem-dibromovinyl systems. The protocol is general and practical, affording a variety of the indole-incorporated products in good to excellent yields even under air atm.

Organic & Biomolecular Chemistry 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 C7H14N4, Formula: C8H5F3O3.

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

Yu, Zhipeng published the artcilePotential mechanisms of the anti-hypertensive effects of RVPSL on spontaneously hypertensive rats using non-targeted serum metabolomics, Recommanded Product: 4-Propylphenol, the publication is Food & Function (2021), 12(18), 8561-8569, database is CAplus and MEDLINE.

The study aimed to investigate potential mechanisms for the anti-hypertensive effects of RVPSL on spontaneously hypertensive rats (SHRs) using a non-targeted metabonomic approach. In this study, UPLC/MS-based non-targeted metabolomics was performed to discover metabolite variation of serum in SHRs with RVPSL treatment. As a result, the serum metabolites of SHRs that were administered RVPSL for four weeks exhibited distinct alterations. Nine potential biomarkers, i.e., choline, adenosine, adrenic acid, L-tryptophan, niacinamide, glycocholic acid, propiolic acid, D-glyceraldehyde 3-phosphate, and phosphoglycolic acid, were significantly altered, which were mainly involved in lipid metabolism, vitamin and amino acid metabolism, purine metabolism, the MAPK signaling pathway, and the renin-angiotensin system. This study suggested that RVPSL potentially exerted potent effects of alleviating hypertension in the SHRs mainly via integrated regulations of metabolism and production of choline, L-tryptophan, nicotinamide, and adenosine.

Food & Function published new progress about 645-56-7. 645-56-7 belongs to alcohols-buliding-blocks, auxiliary class Liquid Crystal &OLED Materials, name is 4-Propylphenol, and the molecular formula is Al2H32O28S3, Recommanded Product: 4-Propylphenol.

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