Month: January 2022

Authors Randolph, JT; Voight, EA; Greszler, SN; Uno, BE; Newton, JN; Gleason, KM; Stolarik, D; Van Handel, C; Bow, DAJ; DeGoey, DA in AMER CHEMICAL SOC published article about PROTEASE INHIBITORS; PHARMACOKINETICS; GLECAPREVIR; NUCLEOSIDE; DESIGN; SAFETY; SINGLE in [Randolph, John T.; Voight, Eric A.; Greszler, Stephen N.; Uno, Brice E.; Newton, James N.; Gleason, Kenneth M.; Stolarik, DeAnne; Van Handel, Cecilia; Bow, Daniel A. J.; DeGoey, David A.] Abbvie Inc, Global Pharmaceut Res & Dev, N Chicago, IL 60064 USA in 2020, Cited 26. Recommanded Product: 87-41-2. The Name is Isobenzofuran-1(3H)-one. Through research, I have a further understanding and discovery of 87-41-2

A research program to discover solubilizing prodrugs of the HCV NS5A inhibitor pibrentasvir (PIB) identified phosphomethyl analog 2 and trimethyl-lock (TML) prodrug 9. The prodrug moiety is attached to a benzimidazole nitrogen atom via an oxymethyl linkage to allow for rapid and complete release of the drug for absorption following phosphate removal by intestinal alkaline phosphatase. These prodrugs have good hydrolytic stability properties and improved solubility compared to PIB, both in aqueous buffer (pH 7) and FESSIF (pH 5). TML prodrug 9 provided superior in vivo performance, delivering high plasma concentrations of PIB in PK studies conducted in mice, dogs, and monkeys. The improved dissolution properties of these phosphate prodrugs provide them the potential to simplify drug dosage forms for PIB-containing HCV therapy.

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Reference:
Benzofuran – Wikipedia,
,Benzofuran | C8H6O – PubChem

COA of Formula: C8H6O2. Recently I am researching about 2-AMINOTHIAZOLE DERIVATIVES; ANTIVIRAL ACTIVITY; ALPHA; POTENT; DISCOVERY; ADIPOGENESIS; METABOLISM; BENZAMIDES; INDOLES; ACID, Saw an article supported by the . Published in PERGAMON-ELSEVIER SCIENCE LTD in OXFORD ,Authors: Mourad, AAE; Mourad, MAE. The CAS is 87-41-2. Through research, I have a further understanding and discovery of Isobenzofuran-1(3H)-one

Aims: Partial PPAR gamma agonists attracted substantially heightened interest as safer thiazolidinediones alternatives. On the other hand, Wnt/beta-catenin antagonists have been highlighted as promising strategy for type 2 diabetes management via up-regulating PPAR gamma gene expression. We aimed at synthesizing novel partial PPAR gamma agonists with beta-catenin inhibitory activity which could enhance insulin sensitivity and avoid the side effects of full PPAR gamma agonists. Main methods: We synthesized novel series of alpha-phthlimido-o-toluoyl-2-aminothiazoles hybrids for evaluating their antidiabetic activity and discovering its mechanistic pathway. We assessed effect of the new hybrids on PPAR gamma activation using a luciferase reporter assay system. Moreover, intracellular triglyceride levels, gene levels of c/EBP alpha, PPAR gamma and PPAR gamma targets including GLUT4, adiponectin, aP2 were measured in 3T3-L1 cells. Uptake of 2-DOG together with PPAR gamma and beta-catenin protein levels were evaluated in 3T3-L1cells. In addition, molecular docking studies with PPAR gamma LBD, physicochemical properties and structure activity relationship of the novel hybrids were also studied. Key findings: Three of the synthesized hybrids showed partial PPAR gamma agonistic activity and distinct PPAR gamma binding pattern. These compounds modulated PPAR gamma gene expression and PPAR gamma target genes; and increased glucose uptake in 3T3-L1 and slightly induced adipogenesis compared to rosiglitazone. Moreover, these compounds reduced beta-catenin protein level which reflected in increased both PPAR gamma gene and protein levels that leads to improved insulin sensitivity and increased GLUT4 and adiponectin gene expression. Significance: Our synthesized compounds act as novel partial PPAR gamma agonists and beta-catenin inhibitors that have potent insulin sensitizing activity and mitigate the lipogenic side effects of TZDs.

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Reference:
Benzofuran – Wikipedia,
,Benzofuran | C8H6O – PubChem

An article Synthesis and Anticancer Activity of Some Fused Heterocyclic Compounds Containing Pyrazole Ring WOS:000536394900001 published article about NATIONAL-CANCER-INSTITUTE; DRUG DISCOVERY; CELL-LINES in [Hassan, A. Y.; Abdel-Aziem, A.; Hussain, A. O.] Al Azhar Univ, Chem Dept, Fac Sci, Girls Branch, POB 11754,Yousef Abbas Str, Cairo, Egypt; [Mohamed, M. A.] Al Azhar Univ, Girls Branch, Fac Sci, Biochem Div,Chem Dept, Cairo, Egypt in 2020, Cited 25. Safety of Isobenzofuran-1(3H)-one. The Name is Isobenzofuran-1(3H)-one. Through research, I have a further understanding and discovery of 87-41-2

5-Amino-1-phenyl-1H-pyrazole-4-carbohydraizde(1) was used as a key to synthesize new imidazopyrazol-5(1H)-one 5, pyrazolopyrimidines 7 and 9. Furthermore, imidazopyrazoles 13, 15, pyrazolopyridine 16 and pyrazolopyrazolopyridopyrimidine 17 were prepared from pyrazoles 10 and 11. The structure of the new compounds was confirmed by spectral data as well as elemental analysis. Some compounds were selected by the national cancer institute NCI (USA) for anticancer activity against different human cancer cell lines. The results indicated that compound 12 exhibited strong anticancer activity toward Renal Cancer UO-31(GI, 42.81%), while compound 3 was strong active against Breast Cancer MCF7 (GI, 49.88%) and moderate against T-47D (GI, 38.15%) cell lines. However, compound 17 showed strong activity against Leukemia CCRF-CEM (GI, 41.37%) and SR (GI, 44.95%), whereas, compound 9 showed weak activity toward all tested cancer cell lines.

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Reference:
Benzofuran – Wikipedia,
,Benzofuran | C8H6O – PubChem

An article Rapid Characterization of Chemical Components in Edible Mushroom Sparassis crispa by UPLC-Orbitrap MS Analysis and Potential Inhibitory Effects on Allergic Rhinitis WOS:000482998900037 published article about MASS-SPECTROMETRY; FATTY-ACIDS; A-D; LIQUID-CHROMATOGRAPHY; KINASE INHIBITOR; FRUITING BODY; IDENTIFICATION; ANTIOXIDANT; HANABIRATAKE; METABOLITES in [Wang, Zhixin; Zhong, Xiangjian; Li, Jinjie; Wang, Xin; Ji, Linlin; Shang, Xiaoya] Beijing Union Univ, Beijing Key Lab Bioact Subst & Funct Food, 191 Beitucheng West Rd, Beijing 100191, Peoples R China; [Liu, Jingyu] Shanxi Agr Univ, Coll Food Sci & Engn, 1 Mingxian South Rd, Jinzhong 030801, Taigu County, Peoples R China in 2019, Cited 108. The Name is Isobenzofuran-1(3H)-one. Through research, I have a further understanding and discovery of 87-41-2. COA of Formula: C8H6O2

Sparassis crispa is a kind of edible fungus widely grows in the north temperate zone, which shows various medicinal properties. Due to the complexity of chemical constitutes of this species, few investigations have acquired a comprehensive configuration for the chemical profile of it. In this study, a strategy based on ultra-high performance liquid chromatography (UPLC) combined with Orbitrap mass spectrometer (MS) was established for rapidly characterizing various chemical components in S. crispa. Through the summarized MS/MS fragmentation patterns of reference compounds and systematic identification strategy, a total of 110 components attributed to six categories were identified for the first time. Moreover, allergic rhinitis (AR) is a worldwide inflammatory disease seriously affecting human health, and the development of drugs to treat AR has been a topic of interest. It has been reported that the extracts of S. crispa showed obvious inhibitory effects on degranulation of mast cell- and allergen-induced IgE and proinflammatory mediators, but the active components and specific mechanism were still not clear. Src family kinases (SFKs) participate in the initial stage of allergy occurrence, which are considered the targets of AR treatment. Herein, on the basis of that self-built chemical database, virtual screening was applied to predict the potential SFKs inhibitors in S. crispa, using known crystal structures of Hck, Lyn, Fyn, and Syk as receptors, followed by the anti-inflammatory activity evaluation for screened hits by intracellular calcium mobilization assay. As results, sparoside A was directly confirmed to have strong anti-inflammatory activity with an IC50 value of 5.06 +/- 0.60 mu M. This study provides a useful elucidation for the chemical composition of S. crispa, and demonstrated its potential inhibitory effects on AR, which could promote the research and development of effective agents from natural resources.

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Reference:
Benzofuran – Wikipedia,
,Benzofuran | C8H6O – PubChem

Formula: C8H6O2. In 2019 MOLECULES published article about ONE-STEP SYNTHESIS; BENZOIC-ACIDS; CARBOXYLIC-ACIDS; SOFT ACIDS; OXIDASE CATALYSIS; INTERNAL ALKYNES; H ALKENYLATIONS; BASES HSAB; ALDEHYDES; KETONES in [Renzetti, Andrea; Fukumoto, Kozo] Univ Ryukyus, Fac Educ, 1 Senbaru, Nishihara, Okinawa 9030213, Japan in 2019, Cited 68. The Name is Isobenzofuran-1(3H)-one. Through research, I have a further understanding and discovery of 87-41-2.

Phthalides and ,-butenolides are two related classes of oxygenated heterocycles with a wide range of biological activities. An innovative strategy to prepare these compounds is based on CH bond functionalization reactions, in which two simple, unfunctionalized molecules are coupled together with cleavage of a CH bond and formation of a CX bond (X=C or heteroatom). This paper reviews the methods for the synthesis of phthalides and ,-butenolides by CH bond functionalization from non-halogenated starting materials. Over 30 methods are reported, mostly developed during the past ten years.

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Reference:
Benzofuran – Wikipedia,
,Benzofuran | C8H6O – PubChem

An article Light elicited growth, antioxidant enzymes activities and production of medicinal compounds in callus culture of Cnidium officinale Makino WOS:000476964700006 published article about CELL-CULTURES; IN-VITRO; REGENERATION; QUALITY; DIFFERENTIATION; METABOLISM; PHTHALIDES; INDUCTION; CAPACITY; STRESS in [Adil, Muhammad; Jeong, Byoung Ryong] Gyeongsang Natl Univ, Inst Agr & Life Sci, Jinju 52828, South Korea; [Ren, Xiuxia; Jeong, Byoung Ryong] Gyeongsang Natl Univ, Div Appl Life Sci, Dept Hort, Grad Sch,BK Plus Program 21, Jinju 52828, South Korea; [Jeong, Byoung Ryong] Gyeongsang Natl Univ, Res Inst Life Sci, Jinju 52828, South Korea; [Adil, Muhammad] Univ Karachi, Int Ctr Chem & Biol Sci, HEJ Res Inst Chem Biotechnol Wing, Karachi 75270, Pakistan in 2019, Cited 45. The Name is Isobenzofuran-1(3H)-one. Through research, I have a further understanding and discovery of 87-41-2. Name: Isobenzofuran-1(3H)-one

Cnidium officinale Makino is an important medicinal plant of oriental clinics and is considered as the main source of phthalides, polyphenols, and flavonoids. However, there is no available report regarding the effect of different light colors on the secondary metabolites composition of C. officinale. In this study different light (dark, white, blue, red and red: blue) conditions were arranged to raise callus on MS medium containing 0.5 mg.L-1 of each 2,4-D and BAP. Callus grown in dark condition showed maximum (2.0 g) fresh weight with lower total phenolic and flavonoids contents. Also, in dark condition callus faced higher catalase (CAT) and guaiacol peroxidase (GPX) activities to avoid free radicals. Mix (red: blue) light condition favored the synthesis of phenolics and flavonoids in callus at the cost of higher ascorbate peroxidase (APX) and superoxide dismutase (SOD) enzymes expression. However, DPPH free radical scavenging activity was less variable among the samples from the different light conditions. Interestingly, the HPLC profile showed higher (28.3 mu g.g(-1) DW) phthalide accumulation in dark grown-cultures. Compared to other light conditions, 3-butyledinephthalide accumulation was higher (0.43 mu g-g(-1) DW) in white light-grown callus. These findings suggest that light conditions play an important role in the regulation of in vitro callus growth and synthesis of important medicinal compounds of C. officinale.

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Reference:
Benzofuran – Wikipedia,
,Benzofuran | C8H6O – PubChem

Collin, DE; Folgueiras-Amador, AA; Pletcher, D; Light, ME; Linclau, B; Brown, RCD in [Collin, Diego E.; Folgueiras-Amador, Ana A.; Pletcher, Derek; Light, Mark E.; Linclau, Bruno; Brown, Richard C. D.] Univ Southampton, Sch Chem, Southampton SO17 1BJ, Hants, England published Cubane Electrochemistry: Direct Conversion of Cubane Carboxylic Acids to Alkoxy Cubanes Using the Hofer-Moest Reaction under Flow Conditions in 2020, Cited 64. Category: benzofurans. The Name is Isobenzofuran-1(3H)-one. Through research, I have a further understanding and discovery of 87-41-2.

The highly strained cubane system is of great interest as a scaffold and rigid linker in both pharmaceutical and materials chemistry. The first electrochemical functionalisation of cubane by oxidative decarboxylative ether formation (Hofer-Moest reaction) was demonstrated. The mild conditions are compatible with the presence of other oxidisable functional groups, and the use of flow electrochemical conditions allows straightforward upscaling.

Welcome to talk about 87-41-2, If you have any questions, you can contact Collin, DE; Folgueiras-Amador, AA; Pletcher, D; Light, ME; Linclau, B; Brown, RCD or send Email.. Category: benzofurans

Reference:
Benzofuran – Wikipedia,
,Benzofuran | C8H6O – PubChem

An article EXPLORATION OF MODERATE CONDITIONS AND SUBSTRATE VARIATION IN THE DIRECT CONDENSATION BETWEEN PHTHALIDE AND PRIMARY AMINE CATALYZED BY GaCl3. ARE ALIPHATIC AMINES LESS REACTIVE THAN AROMATIC ONES? WOS:000474679300017 published article about CONDITION PHTHALIMIDINE SYNTHESIS; DUAL SYNTHETIC AUXILIARIES; 1,2,3-1H-BENZOTRIAZOLE; 2-MERCAPTOETHANOL; ISOINDOLINONES; MECHANISM in [Takahashi, Ichiro; Nishiwaki, Yoshinori; Saitoh, Kenta; Matsunaga, Takatoshi; Aratake, Akihiro; Morita, Toshio] Univ Fukui, Fac Engn, Dept Appl Chem & Biotechnol, Bunkyo Ku, Fukui 9108507, Japan; [Hosoi, Shinzo] Kyoto Pharmaceut Univ, Res Ctr Pharm Educ, Yamashina Ku, 5 Nakauchi Cho, Kyoto 6078414, Japan in 2019, Cited 38. The Name is Isobenzofuran-1(3H)-one. Through research, I have a further understanding and discovery of 87-41-2. HPLC of Formula: C8H6O2

Direct condensation between phthalide and a primary amine in the presence of Lewis acid was achieved for the first time in organic solvent-diluted reaction systems catalyzed by GaCl3. The peripheral aspects of this reaction is discussed.

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Reference:
Benzofuran – Wikipedia,
,Benzofuran | C8H6O – PubChem

Ogawa, N; Furukawa, S; Kosugi, Y; Takazawa, T; Kanomata, N in [Ogawa, Narihito; Kosugi, Yuya; Takazawa, Takayuki] Meiji Univ, Dept Appl Chem, Kawasaki, Kanagawa 2148571, Japan; [Furukawa, Sei; Kanomata, Nobuhiro] Waseda Univ, Dept Chem & Biochem, Shinjuku Ku, Tokyo 1698555, Japan published Biomimetic systems involving sequential redox reactions in glycolysis – the sulfur effect in 2020, Cited 22. Quality Control of Isobenzofuran-1(3H)-one. The Name is Isobenzofuran-1(3H)-one. Through research, I have a further understanding and discovery of 87-41-2.

Magnesium hemithioacetates were used as model cysteine compounds to mimic natural hemithioacetals, and their biomimetic oxidation reactions using a model NAD(+) compound were investigated. Cyclic hemithioacetate was found to be the best substrate for the reaction with the model NAD(+) compound, which gave the corresponding NADH analog in excellent yield.

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Reference:
Benzofuran – Wikipedia,
,Benzofuran | C8H6O – PubChem

An article Formates plus triazabicyclodecene (TBD): an efficient platform for non-gaseous carbonylation and unexpected hydrogenation WOS:000466794900010 published article about PALLADIUM-CATALYZED CARBONYLATION; METAL-FREE CONSTRUCTION; ARYL HALIDES; N-FORMYLSACCHARIN; EX-SITU; CO; HYDROESTERIFICATION; AMINOCARBONYLATION; ALKYNES; SEQUENCE in [Chen, Dianpeng; Yao, Jinzhong; Chen, Linlin; Hu, Linfeng; Zhou, Hongwei] Jiaxing Univ, Coll Biol Chem Sci & Engn, Jiaxing 314001, Zhejiang, Peoples R China; [Chen, Dianpeng] Qufu Normal Univ, Sch Chem & Chem Engn, Qufu 273165, Shandong, Peoples R China; [Li, Xiaofang] Hunan Univ Sci Technol, Sch Chem & Chem Engn, Xiangtan 411201, Hunan, Peoples R China in 2019, Cited 52. The Name is Isobenzofuran-1(3H)-one. Through research, I have a further understanding and discovery of 87-41-2. Safety of Isobenzofuran-1(3H)-one

A highly efficient palladium-catalyzed TBD-formate system for carbonylation/hydrogenation was reported. Based on the obvious solvent effect and reasonable mechanism study, we achieved tunable carbonylation or hydrogenation. With the advantages of simple operation, mild conditions and storable reagents, this protocol should be of interest not only for synthetic scientists but also helpful for laboratory operators.

Safety of Isobenzofuran-1(3H)-one. Welcome to talk about 87-41-2, If you have any questions, you can contact Chen, DP; Yao, JZ; Chen, LL; Hu, LF; Li, XF; Zhou, HW or send Email.

Reference:
Benzofuran – Wikipedia,
,Benzofuran | C8H6O – PubChem