Day: November 15, 2022

Liang, Shuang published the artcileGC-MS analysis of chemical constituents of volatile oils of the yao medicine Thunbergia grandiflora from different habitats in guangxi, Category: benzothiophene, the main research area is Thunbergia grandiflora guangxi yao medicine volatile oil GCMS.

This study was conducted to compare and anlyze the chem. constituents of the volatile oils of the Yao medicine Thunbergia grandiflora from different habitals.A quarz capillary column DB-1MS, an EI ion source a quadrupole mass analyzer were used for anal. The chromatog. and mass spectrum information obtained was automatically retrieved and analyzed by data processing system and its memory spectrum library (Nist. 08). The relative content of each chem. component in the volatile oil was determinded by the peak area normalization method.Forty nine chromatog. peaks were isolated from the sample produced in Shitun, Bailongtan Town, Mashan County, and 24 chem. constituents were identified, accounting for 88.78% of the total volatile oil. Forty nine chromatog. peaks were isolated from the sample produced in Hongdu Village, Chengjiang Town, Duan County, and 30 chem. constituents were identified, accounting for 88.38% of the total volatile oil. Forty eight chromatog. peaks were isolated from the sample produced in Longwan Township, Du’an County, and 25 chem. constituents were identified, accounting for 80.01% of the total volatile oil. Nine chem. constituents were common to the volatile oils of the samples from the three habitats. It could be seen that the main components of volatile oils from T. grandiflora produced in different areas are different.

Agricultural Biotechnology published new progress about Gas chromatography-mass spectrometry. 1468-83-3 belongs to class benzothiophene, name is 3-Acetylthiophene, and the molecular formula is C6H6OS, Category: benzothiophene.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Zhao, Guozhong published the artcileEffect of wheat bran steam explosion pretreatment on flavors of nonenzymatic browning products, HPLC of Formula: 1468-83-3, the main research area is wheat bran steam explosion flavor nonenzymic browning.

Wheat bran, which contains a large amount of cellulose, is used as a raw material to produce soy sauce, but it is hard to degrade during fermentation Steam explosion (SE) is efficient in hydrolyzing the cellulose for enhancing enzymic digestion and solvent accessibility. In this study, we applied a SE at a sufficiently high pressure to damage the integrity of the wheat bran structure and modify it to assume a layered form. We found that cellulose, hemicellulose, and lignin structures were collapsed by SE pretreatment, which was indicated by their changes in Fourier transform IR spectroscopy (FTIR). The amounts of cellulose, hemicellulose, and lignin decreased by 5.8%, 21.4%, and 43.4%, resp., under 1.5 MPa, resulting in the significant reduction of sugar and amino acid nitrogen. The co-reaction of nonenzymic browning after SE pretreatment resulted in an intense increase in flavor (overall feeling), as determined by electronic nose anal. and sensory evaluation. In conclusion, SE pretreatment under 1.0 MPa was proven to be the most optimal state for the production of aroma compounds (volatile compounds), which are essential for soy sauce production

LWT–Food Science and Technology published new progress about Browning (food) (nonenzymic browning). 1468-83-3 belongs to class benzothiophene, name is 3-Acetylthiophene, and the molecular formula is C6H6OS, HPLC of Formula: 1468-83-3.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Xiao, Miao published the artcileTransition-Metal-Free Hydrogen Autotransfer: Diastereoselective N-Alkylation of Amines with Racemic Alcohols, Application In Synthesis of 1468-83-3, the main research area is diastereoselective alkylation amines alc chiral amine synthesis; alcohols; alkylation; amines; deuterium; reaction mechanisms.

A practical method for the synthesis of α-chiral amines by alkylation of amines with alcs. in the absence of any transition-metal catalysts has been developed. Under the co-catalysis of a ketone and NaOH, racemic secondary alcs. reacted with Ellman’s chiral tert-butanesulfinamide by a hydrogen autotransfer process to afford chiral amines with high diastereoselectivities (up to >99:1) [e.g., 1-phenylethanol + (R)-(+)-tert-butanesulfinamide → I (70%, > 95:5 d.r.) in presence of acetophenone and NaOH in toluene]. Broad substrate scope and up to a 10 g scale production of chiral amines were demonstrated. The method was applied to the synthesis of chiral deuterium-labeled amines with high deuterium incorporation and optical purity, including examples of chiral deuterated drugs. The configuration of amine products is found to be determined solely by the configuration of the chiral tert-butanesulfinamide regardless of that of alcs., and this is corroborated by DFT calculations Further mechanistic studies showed that the reaction is initiated by the ketone catalyst and involves a transition state similar to that proposed for the Meerwein-Ponndorf-Verley (MPV) reduction, and importantly, it is the interaction of the sodium cation of the base with both the nitrogen and oxygen atoms of the sulfinamide moiety that makes feasible, and determines the diastereoselectivity of, the reaction.

Angewandte Chemie, International Edition published new progress about Alkylation catalysts, stereoselective. 1468-83-3 belongs to class benzothiophene, name is 3-Acetylthiophene, and the molecular formula is C6H6OS, Application In Synthesis of 1468-83-3.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Zhang, Fangming published the artcileRh(III)-catalyzed regioselective C-H activation dialkenylation/annulation cascade for rapid access to 6H-isoindolo[2,1-a]indole, Category: benzothiophene, the main research area is isoindoloindole preparation regioselective diastereoselective; aryl indole acrylate dialkenylation cyclization tandem rhodium catalyst.

The 6H-isoindolo[2,1-a]indoles I [R = H, 2-Br, 2-NO2, 1,3-(CH3)2; R1 = H, 9-Me, 8-OMe, 8-F, etc.; R2 = Et, Me, n-Bu, t-Bu, Bn] and II were accessed via a Rh(III)-catalyzed N-H free indole directed C-H activation dialkenylation/annulation cascade in moderate to excellent yields. This protocol also features: reaction procedures that are insensitive to air and moisture, excellent regioselectivity and good functional group tolerance.

RSC Advances published new progress about Alkenylation (stereo-, regioselective). 1468-83-3 belongs to class benzothiophene, name is 3-Acetylthiophene, and the molecular formula is C6H6OS, Category: benzothiophene.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Takakusa, Hideo published the artcileQuantitative assessment of reactive metabolite formation using 35S-labeled glutathione, Synthetic Route of 40180-04-9, the main research area is drug metabolism reactive metabolite determination radiolabeled glutathione.

The metabolic bioactivation of a drug to a reactive metabolite (RM) and its covalent binding to cellular macromols. is believed to be involved in clin. adverse events, including idiosyncratic drug toxicities. Therefore, it is important to assess the potential of drug candidates to generate RMs and form drug-protein covalent adducts during lead optimization processes. In this study, the RM formation of some marketed drugs were quant. assessed by means of a sensitive and robust detection method that we have established using 35S-glutathione (35S-GSH) as a trapping agent. Problematic drugs well-known to generate RMs exhibited a relatively high rate of 35S-GS-adducts to RM (RM-GS) formation, which contrasted with safe drugs. For practical use in lead optimization processes, a series of new chem. entities were tested and hints on the structural modifications needed in order to minimize their RM formation were provided. Furthermore, the RM-GS formation rates of a number of compounds were compared using their in vitro covalent binding yields to liver proteins determined with 14C-labeled compounds, demonstrating that the RM-GS formation rate could be a substitute for the covalent binding yield within the same series of compounds

Drug Metabolism and Pharmacokinetics published new progress about Drug metabolism (metabolic bioactivation). 40180-04-9 belongs to class benzothiophene, name is 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, and the molecular formula is C13H8Cl2O4S, Synthetic Route of 40180-04-9.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Bauer, John H. published the artcileEffects of diuretic and propranolol on plasma lipoprotein lipids, Formula: C13H8Cl2O4S, the main research area is diuretic propranolol plasma lipoprotein.

To define the effects of diuretics on plasma lipoproteins, experiments were performed in hypertensive subjects after placebo therapy, 4 wk after therapy with either hydrochlorothiazide (HCTZ)(I) [58-93-5] or ticrynafen (TCNF)(II) [40180-04-9], 3 mo after diuretic with propranolol (III) [525-66-6], and 1 mo after therapy with propranolol alone. Plasma lipoproteins were separated by ultracentrifugation and the lipid fractions isolated by extraction and silicic acid thin-layer chromatog. Plasma low-d. lipoprotein (LDL) total cholesterol fell and high-d. lipoprotein (HDL) total cholesterol rose in subjects receiving TCNF. TCNF had no effect on plasma very low-d. lipoprotein (VLDL) triglyceride or phospholipid. There were no significant changes in LDL or HDL total cholesterol in subjects on HCTZ. HCTZ tended to increase plasma VLDL triglyceride and phospholipid. The addition of propranolol to either diuretic had no effect on LDL or HDL total cholesterol but increased VLDL triglyceride, especially in subjects on HCTZ. Propranolol alone had no effect on any of the lipids measured.

Clinical Pharmacology & Therapeutics (St. Louis, MO, United States) published new progress about Lipoproteins Role: BIOL (Biological Study). 40180-04-9 belongs to class benzothiophene, name is 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, and the molecular formula is C13H8Cl2O4S, Formula: C13H8Cl2O4S.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Luo, Wenjun published the artcileSynthesis of W-Phos Ligand and Its Application in the Copper-Catalyzed Enantioselective Addition of Linear Grignard Reagents to Ketones, SDS of cas: 1468-83-3, the main research area is ketone Grignard reagent copper phosphine enantioselective regioselective addition; chiral tertiary alc preparation; Alcohols; Asymmetric Catalysis; Copper; Grignard Reagents; Ketones.

A novel family of PNP ligands (W-Phos) was designed and applied in copper-catalyzed asym. addition of linear Grignard reagents to aryl alkyl ketones, allowing facile access to versatile chiral tertiary alcs. in good to high yields with excellent enantioselectivities (up to 94% yield, 96% ee). The process was also used to synthesize chiral allylic tertiary alcs. from more challenging α,β-unsaturated ketones. Notably, the potential utility of this method was demonstrated in the gram-scale synthesis and modification of various densely functionalized medicinally relevant mols.

Angewandte Chemie, International Edition published new progress about Addition reaction catalysts, regioselective. 1468-83-3 belongs to class benzothiophene, name is 3-Acetylthiophene, and the molecular formula is C6H6OS, SDS of cas: 1468-83-3.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Pons, Catherine published the artcileDetection of human hepatitis anti-liver kidney microsomes (LKM2) autoantibodies on rat liver sections is predominantly due to reactivity with rat liver P-450 IIC11, SDS of cas: 40180-04-9, the main research area is cytochrome P450 hepatitis autoantibody.

Anti-liver kidney microsomes (anti-LKM2) autoantibodies, appearing in patients treated with tienilic acid and suffering from hepatitis, react with proteins in rat liver sections. The nature of the rat proteins responsible for this recognition and detection of anti-LKM2 has been investigated. Immunoblot testing of the anti-LKM2 with liver microsomes from diversely treated rats and with purified rat liver cytochromes P 450 (IA1, IA2, IIB1, IIB2, IIC6, IIC11 and IVA1) showed that these antibodies cross-reacted with cytochrome P450IIC11 and also with phenobarbital-induced cytochromes P450IIB1 and IIB2. Moreover, metabolic activation of tienilic acid and of a tienilic acid isomer by untreated rat liver microsomes was partially inhibited by anti-LKM2. On the other hand, monospecific polyclonal anti-rat P450IIC11 antibodies cross-reacted with human microsomal cytochromes P 450 and recognized the same cytochromes P 450 as anti-LKM2. This antibody also gave an immunofluorescence pattern on rat and mouse liver and kidney sections very similar to anti-LKM2. The data presented here show that anti-LKM2 recognize epitope shared by rat P 450 IIC11, and a human P 450 of the family IIC. All the results indicate rat P 450 IIC11, the major isoenzyme present in normal adult male rat liver, as the main antigen recognized by human anti-LKM2 autoantibodies; this is the basis of the immunofluorescence test for detection of these antibodies.

Journal of Pharmacology and Experimental Therapeutics published new progress about Autoantibodies Role: BIOL (Biological Study). 40180-04-9 belongs to class benzothiophene, name is 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, and the molecular formula is C13H8Cl2O4S, SDS of cas: 40180-04-9.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Beaune, P. published the artcileHuman anti-endoplasmic reticulum autoantibodies appearing in a drug-induced hepatitis are directed against a human liver cytochrome P-450 that hydroxylates the drug, Quality Control of 40180-04-9, the main research area is cytochrome P450 autoantibody drug hepatitis.

Anti-liver/kidney microsome (anti-LKM) autoantibodies were found in the serum of patients with cryptogenic chronic hepatitis and with immunoallergic drug-induced hepatitis, such as those induced by halothane or by tienilic acid (called anti-LKM2 in this case). So far the nature of the human microsomal macromols. recognized by these antibodies has not been determined Here it is shown, by using immunoblot techniques, that among the macromols. present in human adult liver microsomes, one protein called cytochrome P 450-8 is specifically recognized by most sera of patients containing anti-LKM2 antibodies but not by control serum. Human fetal liver microsomes that do not contain cytochrome P 450-8 are not recognized by the anti-LKM2 antibodies. It is also shown that anti-cytochrome P 450-8 antibodies as well as human serum containing anti-LKM2 antibodies specifically inhibit the hydroxylation of tienilic acid by human liver microsomes. These results indicate that anti-LKM2 antibodies appearing in patients with hepatitis and concomitant administration of tienilic acid are directed against a cytochrome P 450 isoenzyme that catalyzes the metabolic oxidation of this drug. This suggests a possible mechanism for the appearance of anti-organelle antibodies in a drug-induced hepatitis.

Proceedings of the National Academy of Sciences of the United States of America published new progress about Autoantibodies Role: BIOL (Biological Study). 40180-04-9 belongs to class benzothiophene, name is 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, and the molecular formula is C13H8Cl2O4S, Quality Control of 40180-04-9.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Beaune, Philippe published the artcileAutoantibodies to cytochrome P-450 during autoimmune hepatitis, Related Products of benzothiophene, the main research area is tienilic acid hepatitis autoantibody cytochrome P450; liver kidney microsome autoantibody drug hepatitis; autoimmune hepatitis autoantibody cytochrome.

Anti-liver/kidney microsomes (anti-LKM) autoantibodies have been found in the serum of patients suffering from different kinds of hepatitis including tienilic acid-induced hepatitis. These autoantibodies were used to study the nature of the macromol. that they recognized. By using immunoblot and immunoinhibition techniques it was shown that these autoantibodies recognized specifically human cytochrome P 450-8 (= P-450 MP or P 450-II C9); this cytochrome P-450 is also responsible for the oxidation of tienilic acid and mephenytoin and produced a reactive metabolite covalently bound to proteins. A simple scheme describing some of the steps leading to the disease is proposed. The study of other autoantibodies seems to show that the scheme which is proposed is rather general.

Colloque INSERM published new progress about Autoantibodies Role: BIOL (Biological Study). 40180-04-9 belongs to class benzothiophene, name is 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, and the molecular formula is C13H8Cl2O4S, Related Products of benzothiophene.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem