Category: alcohols-buliding-blocks

Lin, Jian published the artcileDiscovery and Optimization of Quinolinone Derivatives as Potent, Selective, and Orally Bioavailable Mutant Isocitrate Dehydrogenase 1 (mIDH1) Inhibitors, HPLC of Formula: 622-40-2, the publication is Journal of Medicinal Chemistry (2019), 62(14), 6575-6596, database is CAplus and MEDLINE.

Mutations at the arginine residue (R132) in isocitrate dehydrogenase 1 (IDH1) are frequently identified in various human cancers. Inhibition of mutant IDH1 (mIDH1) with small mols. has been clin. validated as a promising therapeutic treatment for acute myeloid leukemia and multiple solid tumors. Herein, we report the discovery and optimization of a series of quinolinones to provide potent and orally bioavailable mIDH1 inhibitors with selectivity over wild-type IDH1. The X-ray structure of an early lead 24 in complex with mIDH1-R132H shows that the inhibitor unexpectedly binds to an allosteric site. Efforts to improve the in vitro and in vivo absorption, distribution, metabolism, and excretion (ADME) properties of 24 yielded a preclin. candidate 63. The detailed preclin. ADME and pharmacol. studies of 63 support further development of quinolinone-based mIDH1 inhibitors as therapeutic agents in human trials.

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 C6H13NO2, HPLC of Formula: 622-40-2.

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

Song, Xiao-xia published the artcileComparison of the preventive and therapeutic effects of ergometrine maleate, carbetocin and carboprost tromethamine on postpartum hemorrhage caused by uterine asthenia, Application In Synthesis of 58551-69-2, the publication is Guangdong Yixue (2017), 38(18), 2850-2852, 2855, database is CAplus.

This paper discusses the safety and effectiveness of ergometrine maleate, carbetocin and carboprost aminobutyric triol in the prevention and treatment of postpartum hemorrhage caused by uterine asthenia during vaginal delivery. These three drugs are safe and effective when postpartum uterine atony occurs in patients with vaginal delivery. Carbetocin can be used as the first choice for oxytocin combination, but due to their different clin. characteristics, the drug selection should take into account the principle of individualization.

Guangdong Yixue 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 C12H9NO, Application In Synthesis of 58551-69-2.

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

Velu, Sadanandan E. published the artcileTethered Dimer Inhibitors of NAD Synthetase: Parallel Synthesis of an Aryl-Substituted SAR Library, Recommanded Product: 3-Morpholinophenol, the publication is Journal of Combinatorial Chemistry (2005), 7(6), 898-904, database is CAplus and MEDLINE.

The authors previously reported that tethered dimers containing indoles on one end and a permanent pos. charge on the other, using a 6-9 carbon polymethylene tether, provided NAD synthetase inhibitors with impressive antibacterial activities against Gram-positives. Here, the authors report that the Ph ring is a good substitute for indole, and the authors utilize solution-phase parallel synthesis to explore structure-activity relationships for substituents on that ring. General conclusions are that nonpolar substituents are more effective than polar ones and that different positional isomers often have very different enzyme inhibition activities. This latter observation reveals that enzyme activity is sensitive to minor structural changes and suggests that nonspecific detergent actions are not important for the observed effects.

Journal of Combinatorial Chemistry published new progress about 27292-49-5. 27292-49-5 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Benzene,Phenol, name is 3-Morpholinophenol, and the molecular formula is C7H6Cl2, Recommanded Product: 3-Morpholinophenol.

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

Zhang, Tao published the artcileA directive Ni catalyst overrides conventional site selectivity in pyridine C-H alkenylation, Computed Properties of 20880-92-6, the publication is Nature Chemistry (2021), 13(12), 1207-1213, database is CAplus and MEDLINE.

Herein, application of bifunctional N-heterocyclic carbene-ligated Ni-Al catalyst in C3-H alkenylation of pyridines was described. This method overrode the intrinsic C2 and/or C4 selectivity, and provided a series of C3-alkenylated pyridines such as I in 43-99% yields and up to 98:2 C3 selectivity. This method not only allowed a variety of pyridine and heteroarene substrates to be used as the limiting reagent, but was also effective for the late-stage C3 alkenylation of diverse complex pyridine motifs in bioactive mols.

Nature Chemistry published new progress about 20880-92-6. 20880-92-6 belongs to alcohols-buliding-blocks, auxiliary class Other Aliphatic Heterocyclic,Chiral,Alcohol, name is ((3aS,5aR,8aR,8bS)-2,2,7,7-Tetramethyltetrahydro-3aH-bis([1,3]dioxolo)[4,5-b:4′,5′-d]pyran-3a-yl)methanol, and the molecular formula is C25H29N9O3, Computed Properties of 20880-92-6.

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

Ubale, Akash S. published the artcileTransition-Metal-Free Alkylative Aromatization of Tetralones using Alcohols/Amino Alcohols Toward the Synthesis of Bioactive Naphthol and Benzo[e/g]indole Derivatives, Name: 2-Aminobutan-1-ol, the publication is Journal of Organic Chemistry (2022), 87(12), 8104-8117, database is CAplus and MEDLINE.

Herein, the synthesis of bioactive naphthols I (R¹ = H, 6-Br, 6-MeO, 7-MeO; R² = Ph, 3-MeC₆H₄, 2-thienyl, etc.) and II or benzindoles III (R³ = Me, Et, PhCH₂, etc.) and IV by alkylative aromatization of the corresponding 1- and 2-tetralones with alcs. R²CH₂OH or amino alcs. H₂NCHR³CH₂OH in the presence of NaOH using aerobic oxidative cross-coupling protocol is reported. This is a general and transition-metal-free method, which uses an inexpensive base, does not require inert conditions, and furnishes water and hydrogen peroxide as byproducts. Moreover, this method is compatible with a wide substrate scope and showed exclusive regioselectivity.

Journal of Organic Chemistry published new progress about 96-20-8. 96-20-8 belongs to alcohols-buliding-blocks, auxiliary class Amine,Aliphatic hydrocarbon chain,Alcohol, name is 2-Aminobutan-1-ol, and the molecular formula is C10H15NO, Name: 2-Aminobutan-1-ol.

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

Blundell, Toby J. published the artcileEnantiopure and racemic radical-cation salts of B(mandelate)₂^– and B(2-chloromandelate)₂^– anions with BEDT-TTF, Related Products of alcohols-buliding-blocks, the publication is Dalton Transactions (2022), 51(12), 4843-4852, database is CAplus and MEDLINE.

Authors report the first examples of radical-cation salts of BEDT-TTF with spiroborate anions [B(mandelate)₂]^– and [B(2-chloromandelate)₂]^–, synthesized from either enantiopure or racemic bidentate mandelate or chloromandelate ligands. In the salts prepared using enantiopure ligands only one of two diastereoisomers of the spiroborate anion is incorporated, with the boron center having the same stereochem. as the enantiopure ligand. For the racemic salts one racemic pair of spiroborate anions containing an R and an S mandelate ligand is incorporated. In certain solvents helical crystals were obtained when using spiroborate anions with enantiopure ligands. Elec. and magnetic properties, and band structure calculations are reported.

Dalton Transactions published new progress about 90-64-2. 90-64-2 belongs to alcohols-buliding-blocks, auxiliary class Carboxylic acid,Benzene,Alcohol,Natural product, name is 2-Hydroxy-2-phenylacetic acid, and the molecular formula is C8H8O3, Related Products of alcohols-buliding-blocks.

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

Llorente, Briardo published the artcileDownregulation of polyphenol oxidase in potato tubers redirects phenylpropanoid metabolism enhancing chlorogenate content and late blight resistance, Related Products of alcohols-buliding-blocks, the publication is Molecular Breeding (2014), 34(4), 2049-2063, database is CAplus.

Land plants synthesize phenolic compounds involved in plant defense against invading pathogens through the phenylpropanoid pathway. Although not considered as part of the phenylpropanoid pathway, plant polyphenol oxidases (PPOs) are enzymes that catalyze cresolase and catecholase reactions on several phenolic compounds Here, transgenic potato (Solanum tuberosum) tubers with downregulated PPO genes (-PPO) were challenged with the oomycete pathogen Phytophthora infestans to investigate the interactions between PPO, phenylpropanoid metabolism, and disease resistance. We found that pathogen invasiveness was reduced in -PPO lines, while microscopic evidences suggested that the mechanism underlying the defense response involved the participation of phenolic compounds Detailed metabolite-profiling analyses demonstrated that the concentration of metabolites related to the phenylpropanoid pathway and chlorogenate in particular was largely altered in PPO-downregulated tubers. Silencing of PPO caused a shift in metabolism from phenylpropanoid precursors to downstream phenylpropanoid products. The presented results suggest that downregulation of PPO redirects the phenylpropanoid metabolism leading to the accumulation of defensive phenolic compounds in the plant cells, consequently enhancing resistance to the pathogen. These results emphasize the importance of components acting in parallel to canonical metabolic pathway constituents in influencing plant metabolism and reveal new scenarios for modulating the levels of phenolics in crops.

Molecular Breeding published new progress about 526-98-7. 526-98-7 belongs to alcohols-buliding-blocks, auxiliary class Sugar Units,Other Sugar Units, name is (3S,4R,5S)-3,4,5,6-Tetrahydroxy-2-oxohexanoic acid, and the molecular formula is C6H10O7, Related Products of alcohols-buliding-blocks.

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

Vaccher, Vincent published the artcileEuropean interlaboratory comparison investigations (ICI) and external quality assurance schemes (EQUAS) for the analysis of bisphenol A, S and F in human urine: Results from the HBM4EU project, Related Products of alcohols-buliding-blocks, the publication is Environmental Research (2022), 112933, database is CAplus and MEDLINE.

The Human Biomonitoring for Europe initiative (HBM4EU) aims to study the exposure of citizens to chems. and potentially associated health effects. One objective of this project has been to build a network of laboratories able to answer to the requirements of European human biomonitoring studies. Within the HBM4EU quality assurance and quality control scheme (QA/QC), a number of interlaboratory comparison investigations (ICIs) and external quality assurance schemes (EQUASs) were organized to ensure data consistency, comparability and reliability. Bisphenols are among the prioritized substance groups in HBM4EU, including bisphenol A (BPA), bisphenol S (BPS) and bisphenol F (BPF) in human urine. In four rounds of ICI/EQUAS, two target concentration levels were considered, related to around P25 and P95 of the typical exposure distribution observed in the European general population. Special attention was paid to the conjugated phase II metabolites known to be most dominant in samples of environmentally exposed individuals, through the anal. of both native samples and samples fortified with glucuronide forms. For the low level, the average percentage of satisfactory results across the four rounds was 83% for BPA, 71% for BPS and 62% for BPF. For the high level, the percentages of satisfactory results increased to 93% for BPA, 89% for BPS and 86% for BPF. 24 out of 32 participating laboratories (75%) were approved for the analyses of BPA in the HBM4EU project according to the defined criterion of Z-scores for both low and high concentration levels in at least two ICI/EQUAS rounds. For BPS and BPF, the number of qualified laboratories was 18 out of 27 (67%) and 13 out of 28 (46%), resp. These results demonstrate a strong anal. capability for BPA and BPS in Europe, while improvements may be needed for BPF.

Environmental Research 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 C28H52N2O2S2Sn2, Related Products of alcohols-buliding-blocks.

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

Fernandez-Real, Jose-Manuel published the artcileSalicylates increase insulin secretion in healthy obese subjects, HPLC of Formula: 328-90-5, the publication is Journal of Clinical Endocrinology and Metabolism (2008), 93(7), 2523-2530, database is CAplus and MEDLINE.

Context: Conflicting results on the effects of salicylates on glucose tolerance in subjects with normal glucose tolerance or type 2 diabetes have been reported. Objective: The objective of the study was to investigate the effects of a salicylate derivative (triflusal) on insulin sensitivity and insulin secretion. Design, Setting, and Participants: This was a double-blind, randomized, crossover study with three treatment periods corresponding to two dose levels of triflusal and placebo in healthy obese subjects. Main Outcome Measures: Insulin sensitivity and insulin secretion, evaluated through frequently sampled iv glucose tolerance test that was performed after each treatment period, were measured. Insulin secretion was also evaluated in vitro in mice and human islets of Langerhans. Results: The administration of triflusal led to decreased fasting serum glucose concentration in the study subjects. Insulin sensitivity did not significantly change after each treatment period. Insulin secretion, however, significantly increased in a dose-dependent fashion after each triflusal treatment period. The administration of 800 μM of the main triflusal metabolite to whole mice islets of Langerhans led to a sustained increase in intracellular calcium concentration level. This was followed by a significantly increase in insulin secretion. In human islets, 200 μM of 2-hydroxy-4-trifluoromethylbenzoic acid was sufficient to increase insulin release. Conclusions: The administration of a salicylate compound led to lowering of serum glucose concentration We suggest that this effect was mediated through increased insulin secretion induced by salicylate directly on the β-cell.

Journal of Clinical Endocrinology and Metabolism 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, HPLC of Formula: 328-90-5.

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

Mondejar-Lopez, Maria published the artcileBiogenic Silver Nanoparticles from Iris tuberosa as Potential Preservative in Cosmetic Products, Related Products of alcohols-buliding-blocks, the publication is Molecules (2021), 26(15), 4696, database is CAplus and MEDLINE.

Biogenic-silver nanoparticles emerge as new nanosilver platforms that allow us to obtain silver nanoparticles via “green chem.”. In our study, biogenic-silver nanoparticles were obtained from Iris tuberosa leaf extract Nanoparticles were characterized by a UV-vis spectroscopy, dynamical light scattering technique. The transmission electron microscope revealed spheric and irregular nanoparticles with 5 to 50 nm in diameter Antimicrobial properties were evaluated against typical microbial contaminants found in cosmetic products, showing high antimicrobial properties. Furthermore, natural moisturizing cream was formulated with biogenic-silver nanoparticles to evaluate the preservative efficiency through a challenge test, indicating its promising use as preservative in cosmetics.

Molecules published new progress about 70445-33-9. 70445-33-9 belongs to alcohols-buliding-blocks, auxiliary class Aliphatic Chain, name is 3-((2-Ethylhexyl)oxy)propane-1,2-diol, and the molecular formula is C11H24O3, Related Products of alcohols-buliding-blocks.

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