Tag: M.W=250-300

Mayer, Nicole; Schweiger, Martina; Fuchs, Elisabeth; Migglautsch, Anna K.; Doler, Carina; Grabner, Gernot F.; Romauch, Matthias; Melcher, Michaela-Christina; Zechner, Rudolf; Zimmermann, Robert; Breinbauer, Rolf published the artcile< Structure-activity relationship studies for the development of inhibitors of murine adipose triglyceride lipase (ATGL)>, Application of C19H34O2, the main research area is PNPLA2 lipolysis NAFLD atglistatin murine ATGL inhibitors SAR; Atglistatin; Lipolysis; NAFLD; PNPLA2; Small molecule inhibitor.

High serum fatty acid (FA) levels are causally linked to the development of insulin resistance, which eventually progresses to type 2 diabetes and non-alc. fatty liver disease (NAFLD) generalized in the term metabolic syndrome. Adipose triglyceride lipase (ATGL) is the initial enzyme in the hydrolysis of intracellular triacylglycerol (TG) stores, liberating fatty acids that are released from adipocytes into the circulation. Hence, ATGL-specific inhibitors have the potential to lower circulating FA concentrations, and counteract the development of insulin resistance and NAFLD. In this article, we report about structure-activity relationship (SAR) studies of small mol. inhibitors of murine ATGL which led to the development of Atglistatin. Atglistatin is a specific inhibitor of murine ATGL, which has proven useful for the validation of ATGL as a potential drug target.

Bioorganic & Medicinal Chemistry published new progress about Drug targets. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Application of C19H34O2.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Bai, Lei; Huo, Shuhui; Chen, Jing; Lu, Xiaoquan published the artcile< Squaramide fluorescence probe for chiral recognition of α-amino acids>, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is squaramide fluorescence probe chiral recognition alpha amino acid fluorometry.

Four squaramide fluorescence probes were synthesized using natural amino acids as chiral sources, which featured concise synthetic route, simple work-up and purification without column chromatog. The chiral recognition effects of these squaramide probes for phenylalanine, valine and proline were tested using fluorescence spectrum, which indicated that probe 5 could effectively discriminate two enantiomers of phenylalanine. The fluorescence intensity of probe 5 was remarkably enhanced after adding L-phenylalanine. On the contrary, it was observably reduced when D-phenylalanine was added, and the fluorescence intensity ratio of two enantiomers (IL/ID) was up to 2.4.

Gaodeng Xuexiao Huaxue Xuebao published new progress about Chiral recognition. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Postigo, Al published the artcile< Propagation chains in photocatalyzed radical nucleophilic substitutions of thiolates with perfluoroalkyl groups>, Synthetic Route of 4098-06-0, the main research area is thiol perfluorobutyl iodide perfluoroalkylation mecahnism quantum yield fluorescence quenching.

Quantum yields and radical chain lengths were investigated in photocatalyzed radical nucleophilic perfluorobutyl group substitution reactions of 2-mercaptothiolate anion under three different photocatalytic systems operating in reductive and quenching manners. Important propagation chain lengths were uncovered with photocatalysts under both scenarios, reductive and oxidative. The different overall quantum yields and chain lengths observed demonstrated the balance between the efficiency of the photoinitiation events, propagation and termination steps. Theor. calculations provide a better understanding and throw light into whether a closed or an open catalytic cycle is operating in photoinitiated perfluoroalkyl group-thiolate coupling reaction.

Chemical Physics Letters published new progress about Chemical chains. 4098-06-0 belongs to class esters-buliding-blocks, and the molecular formula is C12H16O7, Synthetic Route of 4098-06-0.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Meng, Xianglong; Yan, Jingning; Ma, Junnan; Kang, An Na; Kang, Seok Yong; Zhang, Qi; Lyu, Chenzi; Park, Yong-Ki; Jung, Hyo Won; Zhang, Shuosheng published the artcile< Effects of Jowiseungki-tang on high fat diet-induced obesity in mice and functional analysis on network pharmacology and metabolomics analysis>, Electric Literature of 112-63-0, the main research area is diabetes mellitus obesity Jowiseungki tang metabolomics pharmacol; Diabetes mellitus; High fat diet; Jowiseungki-tang; Metabolomics; Network pharmacology.

In traditional Chinese and Korean medicine, Jowiseungki-tang (JST) is a prescription for diabetes mellitus (DM) treatment. However, little scientific evidence is known of its effect in diabetic condition. We assessed the effects of JST on high-fat diet (HFD)-induced obesity with inflammatory condition in mice and to analyze the therapeutic function of JST on network pharmacol. as well as targeted metabolomics. JST administration at 100 mg/kg and 500 mg/kg for a period of 4 wk in HFD-induced obese mice, body weight gain, energy utility, calorie intake, and levels of glucose, insulin, total cholesterol, triglyceride, LDL-cholesterol as well as interleukin-6 were measured. Measurements of HDL-cholesterol (HDL-C) were performed and compared to those of the control group. Moreover, the therapeutic function of JST on obesity was analyzed furtherly based on network pharmacol. and targeted metabolomics methods. Administration of JST at 100 mg/kg and 500 mg/kg for a period of 4 wk in HFD-induced obesity mice significantly decreased the body weight gain, energy utility, calorie intake, and levels of insulin, total cholesterol, LDL-cholesterol, triglyceride, and interleukin-6. However, HDL-cholesterol (HDL-C) levels showed marked elevation relative to control groups. JST administration strongly inhibited expressions of inducible nitric oxide synthase, inflammatory proteins, and cyclooxygenase-2 in the pancreas, stomach, and liver tissues, and reduced hepatic steatosis and pancreatic hyperplasia. In network pharmacol. anal., the putative functional targets of JST are underlie on modulation of cofactor-, coenzyme-, and fatty acid-bonding, insulin resistance, and inflammatory response, fine-tuned the phosphatase binding and signal pathway activation, such as mitogen activated protein kinases, phosphatidylinositol 3-kinases/protein kinase B, protein kinase C, and receptor of glycation end products as well-advanced glycation end products. According to the metabolomics anal., the contents and energy metabolites, and medium and long chain fatty acids was significantly changed in mice pancreases. JST is a valuable prescription for treatment of patients with DM in traditional clinics through inhibition of obesity, inflammatory condition and metabolism

Journal of Ethnopharmacology published new progress about Albumins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Electric Literature of 112-63-0.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Rout, Deeptimayee; Dash, Umesh Chandra; Kanhar, Satish; Swain, Sandeep Kumar; Sahoo, Atish Kumar published the artcile< Homalium zeylanicum attenuates streptozotocin-induced hyperglycemia and cellular stress in experimental rats via attenuation of oxidative stress imparts inflammation>, Name: (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is Homalium hyperglycemia leaf oxidative stress inflammation; 8-OHdG; CRP; Homalium zeylanicum; TNF-α; α-amylase; α-glucosidase.

Homalium zeylanicum (Gardner) Benth (Salicaceae) leaves are being used as folklore medicine to treat diabetes by the local folk of Andhra Pradesh, India. The medicinal claim of this plant with hypoglycemic effects was initially studied by the authors. Antioxidant activities of the hydroalc. fraction of leaves of H. zeylanicum leaves (HAHZL) were pos. correlated with phenols and flavonoids contents. Based on the previous findings, addnl. research is needed to examine the efficacy of using HAHZL to treat hyperglycemia. We therefore investigated in vitro and in vivo glycemic response of HAHZL, and evaluation of possible mechanism of bioactive mols. in mitigating streptozotocin-induced cellular stress in exptl. rats via attenuation of oxidative stress imparts inflammation. GC-MS/MS anal. of HAHZL was carried out to identify bioactive constituents. In vitro antidiabetic (α-glucosidase, α-amylase) and anti-inflammatory activities were investigated. HFD/low-STZ-prompted diabetic Wistar rats were administered with HAHZL (300 and 400 mg/kg; oral) for 28 days. Blood serum, oxidative stress, inflammation, DNA damage, and antidiabetic markers of pancreas and liver were determined Histopathol. studies of liver and pancreas were performed to assess the protective role of HAHZL. GC-MS/MS study revealed 7 bioactive compounds e.g., Phenol, 4-ethenyl-, acetate (28.68%), hydroquinone (9.10%), n-hexadecanoic acid (0.55%), phytol (0.57%), arbutin (17.65%), Vitamin E (1.04%), β-Sitosterol (1.54%) which possess antioxidant, anti-inflammatory and anti-diabetic activities. HAHZL showed significant in vitro glycemic response as evidenced by the inhibition of α-amylase, and α-glucosidase activities. Lineweaver-Burk plot revealed that HAHZL exhibited competitive and mixed competitive inhibition towards α-amylase and α-glucosidase, resp. HAHZL at 400 mg/kg modulated the pathophysiol. associated with HFD/STZ-induced type2 diabetes mellitus and significantly (p < 0.001) improved antihyperglycemic (SG, SI, HOMA-IR, and HbA1C), antidyslipidemic (TC, HDL-C, LDL-C, and TG), antioxidative (MDA, SOD, CAT, GSH, and 8-OHdG) and anti-inflammatory (TNF-α, and CRP) markers in serum, pancreas and liver. In vitro and in vivo test results were corroborated by the improvement of pancreatic and hepatic tissue architecture in diabetic rats. HAHZL bearing bioactive components phenol, 4-ethenyl-,acetate, hydroquinone, n-hexadecanoic acid, arbutin, phytol, vitamin E and β-sitosterol balanced glycemic level by normalizing the levels of glycemic indexes, lipid profile, pancreas and liver functional markers in STZ-induced T2DM rats. Journal of Ethnopharmacology published new progress about Anti-inflammatory agents. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Name: (9Z,12Z)-Methyl octadeca-9,12-dienoate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Diaz-Navarro, Marta; Bolivar, Paula; Andres, Maria Fe; Gomez-Munoz, Maria Teresa; Martinez-Diaz, Rafael A.; Valcarcel, Felix; Garcia-Paris, Mario; Bautista, Luis M.; Gonzalez-Coloma, Azucena published the artcile< Antiparasitic Effects of Potentially Toxic Beetles (Tenebrionidae and Meloidae) from Steppe Zones>, COA of Formula: C19H34O2, the main research area is Blaps Mylabris Aspergillus Hyalomma myristic acid methyl linoleate antiparasitic; GCMS; Meloidae; Tenebrionidae; antiprotozoal; cantharidin; ethyl oleate; nematicide; otididae.

Arthropods and specifically beetles can synthesize and/or sequester metabolites from dietary sources. In beetle families such as Tenebrionidae and Meloidae, a few studies have reported species with toxic defensive substances and antiparasitic properties that are consumed by birds. Here we have studied the antiparasitic activity of extracts from beetle species present in the habitat of the Great Bustard (Otis tarda) against four pathogen models (Aspergillus niger, Meloidogyne javanica, Hyalomma lusitanicum, and Trichomonas gallinae). The insect species extracted were Tentyria peiroleri, Scaurus uncinus, Blaps lethifera (Tenebrionidae), and Mylabris quadripunctata (Meloidae). M. quadripunctata exhibited potent activity against M. javanica and T. gallinae, while T. peiroleri exhibited moderate antiprotozoal activity. The chem. composition of the insect extracts was studied by gas chromatog. coupled with mass spectrometry (GC-MS) anal. The most abundant compounds in the four beetle extracts were hydrocarbons and fatty acids such as palmitic acid, myristic acid and Me linoleate, which are characteristic of insect cuticles. The presence of cantharidin (CTD) in the M. quadripunctata meloid and Et oleate (EO) in T. peiroleri accounted for the bioactivity of their extracts

Toxins published new progress about Aspergillus niger. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, COA of Formula: C19H34O2.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Chevenier, Emmanuel; Lucatelli, Christophe; Pandya, Urvish; Wang, Wei; Gimbert, Yves; Greene, Andrew E. published the artcile< An anionic polycondensation strategy for the synthesis of dibenzoxanthenones: Progress toward the synthesis of hypoxyxylerone>, Reference of 112-63-0, the main research area is anionic polycondensation dibenzoxanthenone hypoxyxylerone synthesis.

An anionic polycondensation has been used as the key step in a highly convergent strategy for the preparation of hypoxyxylerone derivatives, e.g. I.

Synlett published new progress about Condensation reaction (polycondensation). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Reference of 112-63-0.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Qiu, Di; Mo, Fanyang; Zheng, Zhitong; Zhang, Yan; Wang, Jianbo published the artcile< Gold(III)-catalyzed halogenation of aromatic boronates with N-halosuccinimides>, Reference of 112-63-0, the main research area is halogenation arylboronate halosuccinimide gold trichloride catalyst; regioselective halogenation aryl boronate substituent directed preparation haloaryl boronate; chlorination bromination iodination arylboronate trichlorogold catalyst regioselective preparation haloarylboronate.

Halogenation of aryl boronates ArB(OCMe2)2 (ArBpin) was achieved by reaction with N-halosuccinimide in the presence of 2 mol% of AuCl3; in the same conditions, iron halides, BF3·OEt2 and other common catalysts were proven to be ineffective. Bromination of phenylboronate PhBpin was shown to be non-regioselective, yielding approx. 1:1:1 mixture of 2-Br-, 3-Br-, and 4-BrC6H4Bpin isomers, thus proving a weak ortho-para directing properties of the Bpin substituent. The directing effect of the boronate may be overridden in halogenation of differently substituted benzene derivatives XC6H4Bpin (X = 3-MeO, 2-MeO, 2-Me, 3-Me, 3-OH, 3-Cl, 3-Br, 3-F3CO, 4-Cl) or of disubstituted benzeneboronates X2C6H3Bpin (X2 = 3,5-Me2, 3,5-F2, 3,5-Cl2), which proceeds selectively and with good yields in o- or p-positions to the substituents X. 2- And 3-thiopheneboronates were also halogenated in 5- and 2,5-positions, resp.

Organic Letters published new progress about Aromatic compounds Role: PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Reference of 112-63-0.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Lin, Songwen; Wang, Chunyang; Ji, Ming; Wu, Deyu; Lv, Yuanhao; Zhang, Kehui; Dong, Yi; Jin, Jing; Chen, Jiajing; Zhang, Jingbo; Sheng, Li; Li, Yan; Chen, Xiaoguang; Xu, Heng published the artcile< Discovery and Optimization of 2-Amino-4-methylquinazoline Derivatives as Highly Potent Phosphatidylinositol 3-Kinase Inhibitors for Cancer Treatment>, Synthetic Route of 112-63-0, the main research area is amino methyl quinazoline derivative preparation PI3K inhibitor cancer.

Increased phosphatidylinositol 3-kinase (PI3K) signaling is among the most common alterations in cancer, spurring intensive efforts to develop new cancer therapeutics that target this pathway. In this work, we discovered a series of novel 2-amino-4-methylquinazoline derivatives through a hybridization and subsequent scaffold hopping approach that were highly potent class I PI3K inhibitors. Lead optimization resulted in several promising compounds (e.g., 19, 20, 37, and 43) with nanomolar PI3K potencies, prominent antiproliferative activities, favorable PK profiles, and robust in vivo antitumor efficacies. More interestingly, compared with 19 and 20, 37 and 43 demonstrated improved brain penetration and in vivo efficacy in an orthotopic glioblastoma xenograft model. Furthermore, preliminary safety assessments including hERG channel inhibition, AMES, CYP450 inhibition, and single-dose toxicity were performed to characterize their toxicol. properties.

Journal of Medicinal Chemistry published new progress about Antiproliferative agents. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Synthetic Route of 112-63-0.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Batema, Guido D.; van de Westelaken, Koen T. L.; Guerra, Javier; Lutz, Martin; Spek, Anthony L.; van Walree, Cornelis A.; de Mello Donega, Celso; Meijerink, Andries; van Klink, Gerard P. M.; van Koten, Gerard published the artcile< Luminescent and electronic properties of stilbenoid NCN-pincer PtII compounds>, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is platinum complex preparation crystal structure NMR UV spectra.

A series of 4,4′-disubstituted organic-organometallic stilbenes were synthesized, i.e., the 4′-substituted stilbenoid-NCN-pincer platinum(II) complexes [PtCl(NCN-R-4)] (NCN-R-4 = [C6H2(CH2NMe2)2-2,6-R-4]- in which R = C2H2C6H4-R’-4′ with R’ = NMe2, OMe, SiMe3, H, I, CN, NO2) (1-7). In these compounds the PtCl grouping can be considered to be present as a donor substituent. Their synthesis involved a Horner-Wadsworth-Emmons reaction of [PtCl(NCN-CHO-4)] (9) with the appropriate phosphonate ester derivatives (8a-g). Under these reaction conditions, the C-Pt bond in aldehyde 9 was not affected, and the platinated stilbene products were obtained in 53-90 % yield. The solid state structures of complexes 1, 2 and 5-7 were determined by single-crystal X-ray diffraction, which revealed interesting bent conformations for 2, 5 and 7. Linear correlations were found between both the 13C{1H} (C ipso to Pt) and the 195Pt{1H} NMR chem. shift and the Hammett σp value of the R’ substituent; therefore, these NMR shifts can be used as a qual. probe for the electronic properties of the delocalized π-system to which it is connected. The platinum-stilbene complexes were investigated for charge-transfer properties in solvents of different polarity. The luminescent properties, shown by donor-acceptor complexes 1, 6 and 7, were investigated by fluorescence spectroscopy, and the complexes showed pos. solvatochromism, which indicates dipolar character of the excited state. The excited state lifetimes, which were in the picosecond range, and the quantum yields (ranging from 0.002 to 0.2) were also determined for these complexes. It was established that the presence of the transition metal favors nonradiative decay from the excited state to the ground state.

European Journal of Inorganic Chemistry published new progress about Charge transfer complexes Role: PRP (Properties), SPN (Synthetic Preparation), PREP (Preparation). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics