Day: November 25, 2022

Wang, Ya-Ping published the artcileStudy on the interaction of 3,3-bis(4-hydroxy-1-naphthyl)-phthalide with bovine serum albumin by fluorescence spectroscopy, Synthetic Route of 596-01-0, the publication is Journal of Photochemistry and Photobiology, A: Chemistry (2006), 177(1), 6-11, database is CAplus.

The interaction between 3,3-bis(4-hydroxy-1-naphthyl)-phthalide (NPP) and bovine serum albumin (BSA) have been studied by fluorescence spectroscopy. The binding of NPP quenches the BSA fluorescence. By the fluorescence quenching results, it was found that the binding constant K = 5.30 × 10⁴ L mol^-1, and number of binding sites n = 0.9267. In addition, according to the synchronous fluorescence spectra of BSA, the results showed that the fluorescence spectra of BSA mainly originate from the tryptophan residues. Finally, the distance between the acceptor NPP and BSA was estimated to be 1.94 nm using Foester’s equation on the basis of fluorescence energy transfer. The interaction between NPP and BSA has been verified as consistent with the static quenching procedure and the quenching mechanism is related to the energy transfer.

Journal of Photochemistry and Photobiology, A: Chemistry published new progress about 596-01-0. 596-01-0 belongs to benzofurans, auxiliary class Benzofuran,Naphthalene,Alcohol,Ester, name is 3,3-Bis(4-hydroxynaphthalen-1-yl)isobenzofuran-1(3H)-one, and the molecular formula is C8H14O2, Synthetic Route of 596-01-0.

Referemce:
https://en.wikipedia.org/wiki/Benzofuran,
Benzofuran | C8H6O – PubChem

Qiao, Zongjun published the artcileDirect Cross-Coupling Access to Diverse Aromatic Sulfide: Palladium-Catalyzed Double C-S Bond Construction Using Na₂S₂O₃ as a Sulfurating Reagent, Quality Control of 69626-75-1, the publication is Organic Letters (2014), 16(4), 1212-1215, database is CAplus and MEDLINE.

The Pd-catalyzed cross-coupling of aryl halides, alkyl halides, and Na₂S₂O₃·5H₂O to deliver aromatic thioethers is described. Pyridine, furan, thiophene, benzofuran, benzoxazole, benzothiophene, benzothiazole, and pyrazine are all amenable to this protocol. The odorless and stable solid Na₂S₂O₃·5H₂O was used as a convenient and environmentally friendly source of sulfur. Pd-catalyzed cross-couplings without thiols or thiophenols to build C-S bonds have not previously been achieved, which renders our observation more striking. Thus, e.g., PdCl₂(dppf)/dppf-catalyzed cross coupling of 4-(MeCO)C₆H₄I with nBu-Cl using Na₂S₂O₃·5H₂O and Cs₂CO₃ as base in DMSO/glycol afforded 4-(MeCO)C₆H₄SBu-n in 88% yield.

Organic Letters published new progress about 69626-75-1. 69626-75-1 belongs to benzofurans, auxiliary class Iodide,Benzofuran, name is 2-Iodobenzofuran, and the molecular formula is C8H5IO, Quality Control of 69626-75-1.

Referemce:
https://en.wikipedia.org/wiki/Benzofuran,
Benzofuran | C8H6O – PubChem

Sangu, Kenichiro published the artcileIntermolecular addition reaction to alkenes of acylmolybdenum complexes generated by oxidative addition of aryl or alkenyl halides with molybdenum(0) carbonyl complexes, Formula: C8H5IO, the publication is Synlett (2007), 929-933, database is CAplus.

Acylmolybdenum species, generated by oxidative addition of aryl or alkenyl halides with molybdenum(0) carbonyl complex followed by carbon monoxide insertion, added to various kinds of alkenes intermolecularly to give simple addition products in good yields without formation of carbonylative Heck-type products.

Synlett published new progress about 69626-75-1. 69626-75-1 belongs to benzofurans, auxiliary class Iodide,Benzofuran, name is 2-Iodobenzofuran, and the molecular formula is C8H5IO, Formula: C8H5IO.

Referemce:
https://en.wikipedia.org/wiki/Benzofuran,
Benzofuran | C8H6O – PubChem

Uzumasa, Yasumitsu published the artcileSpectrochemical studies of mixed indicators. II. Absorption spectra of some new mixed indicators in their color-change intervals, Product Details of C28H18O4, the publication is Nippon Kagaku Kaishi (1921-47) (1938), 24-8, database is CAplus.

cf. C. A. 31, 8375.5. The color change of the 5 mixtures, (1) m-cresol purple + xylenol blue, (2) m-cresol purple + thymol blue, (3) xylenol blue + cresolphthalein, (4) α-naphtholphthalein + m-cresol blue, (5) α-naphtholphthalein + cresol red, has been determined in different p_H ranges spectroscopically. It has been shown that the absorption curves of the mixtures can be constructed from those of the components.

Nippon Kagaku Kaishi (1921-47) published new progress about 596-01-0. 596-01-0 belongs to benzofurans, auxiliary class Benzofuran,Naphthalene,Alcohol,Ester, name is 3,3-Bis(4-hydroxynaphthalen-1-yl)isobenzofuran-1(3H)-one, and the molecular formula is C7H7BClFO3, Product Details of C28H18O4.

Referemce:
https://en.wikipedia.org/wiki/Benzofuran,
Benzofuran | C8H6O – PubChem

Fu, Wai Chung published the artcileRegioselective Synthesis of Polycyclic and Heptagon-embedded Aromatic Compounds through a Versatile π-Extension of Aryl Halides, Application of 2-Iodobenzofuran, the publication is Angewandte Chemie, International Edition (2017), 56(25), 7166-7170, database is CAplus and MEDLINE.

A versatile π-extension reaction was developed based on the three-component cross-coupling of aryl halides, 2-haloarylcarboxylic acids, and norbornadiene. The transformation is driven by the direction and subsequent decarboxylation of the carboxyl group, while norbornadiene serves as an ortho-C-H activator and ethylene synthon via a retro-Diels-Alder reaction. Comprehensive DFT calculations were performed to account for the catalytic intermediates.

Angewandte Chemie, International Edition published new progress about 69626-75-1. 69626-75-1 belongs to benzofurans, auxiliary class Iodide,Benzofuran, name is 2-Iodobenzofuran, and the molecular formula is C8H5IO, Application of 2-Iodobenzofuran.

Referemce:
https://en.wikipedia.org/wiki/Benzofuran,
Benzofuran | C8H6O – PubChem

Wang, Zhiren published the artcileDesign, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer’s Disease, Recommanded Product: 5-(6-Hydroxybenzofuran-2-yl)benzene-1,3-diol, the publication is Journal of Medicinal Chemistry (2015), 58(21), 8616-8637, database is CAplus and MEDLINE.

A novel series of clioquinol-moracin hybrids were designed and synthesized by fusing the pharmacophores of clioquinol and moracin M, and their activities as multitarget-directed ligands against Alzheimer’s disease were evaluated. Biol. activity results demonstrated that these hybrids possessed significant inhibitory activities against phosphodiesterase 4D (PDE4D) and Aβ aggregation as well as remarkable antioxidant effects and excellent blood-brain barrier permeability. The optimal compound, I (WBQ5187), exhibited excellent PDE4D inhibitory potency (IC₅₀ = 0.32 μM), significant antioxidant effects, appropriate biometal chelating functions, and interesting properties that modulated self- and metal-induced Aβ aggregation. Two-dimensional NMR studies revealed that I had significant interactions with Aβ_1-42 at the R5, H6, H14, Q15, and F20 residues. Furthermore, this typical hybrid possessed preeminent neuroprotective effects against inflammation in microglial cells. Most importantly, oral administration of I·HCl demonstrated marked improvements in cognitive and spatial memory in a rat model of Alzheimer’s disease and protected hippocampal neurons from necrosis.

Journal of Medicinal Chemistry published new progress about 56317-21-6. 56317-21-6 belongs to benzofurans, auxiliary class Metabolic Enzyme,PDE,Natural product, name is 5-(6-Hydroxybenzofuran-2-yl)benzene-1,3-diol, and the molecular formula is C16H12O, Recommanded Product: 5-(6-Hydroxybenzofuran-2-yl)benzene-1,3-diol.

Referemce:
https://en.wikipedia.org/wiki/Benzofuran,
Benzofuran | C8H6O – PubChem

Minami, Hiroki published the artcileDirect C-C Bond Construction from Arylzinc Reagents and Aryl Halides without External Catalysts, Safety of 2-Iodobenzofuran, the publication is European Journal of Organic Chemistry (2013), 2013(35), 7891-7894, database is CAplus.

A direct cross-coupling between an arylzinc reagent and an aryl halide was accomplished without any external catalyst, enabling efficient and selective formation of the corresponding biaryl compound with broad functional group compatibility. An exchange reaction of (aryl)lithium compounds with zinc chloride gave the desired zinc reactants. The synthesis of the target compounds was achieved using bis(4-methylphenyl)zinc, bis[4-(trifluoromethyl)phenyl]zinc, bis(2-thienyl)zinc, bis(2-benzofuranyl)zinc, etc., as starting materials in a reaction with iodobenzene derivatives The products thus formed included 2-(4-methylphenyl)naphthalene, 2-(2,4,6-trimethylphenyl)naphthalene, 2-(2-naphthalenyl)thiophene, 2-(2-naphthalenyl)benzofuran, 4-methoxy-4′-methyl-1,1′-biphenyl, 4′-methyl[1,1′-biphenyl]-4-carbonitrile and related substances. A reaction of 1-Bromo-4-iodobenzene with bis(2-methylphenyl)zinc gave 2,2”-dimethyl-1,1′:4′,1”-terphenyl.

European Journal of Organic Chemistry published new progress about 69626-75-1. 69626-75-1 belongs to benzofurans, auxiliary class Iodide,Benzofuran, name is 2-Iodobenzofuran, and the molecular formula is C8H5IO, Safety of 2-Iodobenzofuran.

Referemce:
https://en.wikipedia.org/wiki/Benzofuran,
Benzofuran | C8H6O – PubChem

Li, Ruilin published the artcileA combined network pharmacology and molecular biology approach to investigate the active ingredients and potential mechanisms of mulberry (Morus alba L.) leaf on obesity, Recommanded Product: 5-(6-Hydroxybenzofuran-2-yl)benzene-1,3-diol, the publication is Phytomedicine (2021), 153714, database is CAplus and MEDLINE.

As one of traditional Chinese medicine, mulberry leaf is abundant in diverse active ingredients and widely used for the treatment of metabolic disease and its complications. However, there are a few of reports on its application in the prevention and treatment of obesity. And the mol. mechanism on the anti-obesity of mulberry leaf are unknown till now. The present study aimed to evaluate the potential ingredients and targets of mulberry leaf and uncover the anti-obesity mechanisms by using the network pharmacol. tactics and verify its effect by biol. experiments Active ingredients and key targets of mulberry leaf, genes related to obesity were screened through public database. Based on the results of network pharmacol., the flavonoids-enriched fraction of mulberry leaf (MLF) was extracted and composition of this fraction was identified. After that, HepG2 cells model of lipid accumulation was established for verifying the effect of MLF and related mechanisms. A total of 37 active ingredients in mulberry leaf, 192 predicted biol. targets and 8813 obesity-related targets were determined, of which 180 overlapping targets might have obvious curative effects on obesity. The networks showed that mulberry leaf might play a role through key targets, such as AKT, MAPK and IL-6, and regulated PI3K-Akt signaling pathway. Based on HPLC-ESI-QQQ-MS anal., 13 constituents of MLF were identified, including 9 flavonoids. Furthermore, HepG2 cells model of lipid accumulation was established. The results indicated that MLF treatment could down-regulate the secretion of inflammatory cytokines, as well as clearly inhibited lipid droplets formation and alleviated TC, TG, HDL-C and LDL-C levels. Pos. effect was observed on hypolipidemic efficacy due to the regulation of PI3K/Akt/Bcl-xl pathway, as indicated by the amelioration of PI3K, Akt and Bcl-xl gene and protein expression. This study firstly systematically disclose the multi-ingredients, multi-targets mechanisms of mulberry leaf on obesity by using network pharmacol. approach, and validate in HepG2 cells that the protective effect of MLF against obesity involved both inflammation response and lipid metabolism involving PI3K/Akt/Bcl-xl signaling pathway. It provides indications for further mechanistic research of mulberry leaf and also for the development as a potential candidate for the therapy for obese patients.

Phytomedicine published new progress about 56317-21-6. 56317-21-6 belongs to benzofurans, auxiliary class Metabolic Enzyme,PDE,Natural product, name is 5-(6-Hydroxybenzofuran-2-yl)benzene-1,3-diol, and the molecular formula is C14H10O4, Recommanded Product: 5-(6-Hydroxybenzofuran-2-yl)benzene-1,3-diol.

Referemce:
https://en.wikipedia.org/wiki/Benzofuran,
Benzofuran | C8H6O – PubChem

Pflieger, Aude published the artcileNatural stilbenoids isolated from grapevine exhibiting inhibitory effects against HIV-1 integrase and eukaryote MOS1 transposase in vitro activities, SDS of cas: 56317-21-6, the publication is PLoS One (2013), 8(11), e81184/1-e81184/13, 13 pp., database is CAplus and MEDLINE.

Polynucleotidyl transferases are enzymes involved in several DNA mobility mechanisms in prokaryotes and eukaryotes. Some of them such as retroviral integrases are crucial for pathogenous processes and are therefore good candidates for therapeutic approaches. To identify new therapeutic compounds and new tools for investigating the common functional features of these proteins, we addressed the inhibition properties of natural stilbenoids deriving from resveratrol on two models: the HIV-1 integrase and the eukaryote MOS-1 transposase. Two resveratrol dimers, leachianol F and G, were isolated for the first time in Vitis along with fourteen known stilbenoids: E-resveratrol, E-piceid, E-pterostilbene, E-piceatannol, (+)- E-ε-viniferin, E-ε-viniferinglucoside, E-scirpusin A, quadragularin A, ampelopsin A, pallidol, E-miyabenol C, E-vitisin B, hopeaphenol, and isohopeaphenol and were purified from stalks of Vitis vinifera (Vitaceae), and moracin M from stem bark of Milliciaexelsa (Moraceae). These compounds were tested in in vitro and in vivo assays reproducing the activity of both enzymes. Several mols. presented significant inhibition on both systems. Some of the mols. were found to be active against both proteins while others were specific for one of the two models. Comparison of the differential effects of the mols. suggested that the compounds could target specific intermediate nucleocomplexes of the reactions. Addnl. E-pterostilbene was found active on the early lentiviral replication steps in lentiviruses transduced cells. Consequently, in addition to representing new original lead compounds for further modeling of new active agents against HIV-1 integrase, these mols. could be good tools for identifying such reaction intermediates in DNA mobility processes.

PLoS One published new progress about 56317-21-6. 56317-21-6 belongs to benzofurans, auxiliary class Metabolic Enzyme,PDE,Natural product, name is 5-(6-Hydroxybenzofuran-2-yl)benzene-1,3-diol, and the molecular formula is C14H10O4, SDS of cas: 56317-21-6.

Referemce:
https://en.wikipedia.org/wiki/Benzofuran,
Benzofuran | C8H6O – PubChem

Vedantham, Ravindra published the artcileImproved One-Pot Synthesis of Citalopram Diol and Its Conversion to Citalopram, Name: 1-(3-(Dimethylamino)propyl)-1-(4-fluorophenyl)-3-oxo-1,3-dihydroisobenzofuran-5-carbonitrile, the publication is Organic Process Research & Development (2013), 17(5), 798-805, database is CAplus.

An improved process is developed for the preparation of citalopram diol, I which involves two consecutive Grignard reactions in situ followed by an efficient and simple workup process with improved overall yield. Process development efforts for conversion of I·HBr into citalopram, II·HBr, and a control strategy for impurities are discussed. The present work addresses the challenges associated with the process development and scale-up of citalopram such as handling of unstable intermediates, control of various potential impurities, and process safety to achieve an economic and scalable process.

Organic Process Research & Development published new progress about 372941-54-3. 372941-54-3 belongs to benzofurans, auxiliary class Other Aliphatic Heterocyclic,Fluoride,Nitrile,Amine,Benzene,Ester, name is 1-(3-(Dimethylamino)propyl)-1-(4-fluorophenyl)-3-oxo-1,3-dihydroisobenzofuran-5-carbonitrile, and the molecular formula is C3H5F3O, Name: 1-(3-(Dimethylamino)propyl)-1-(4-fluorophenyl)-3-oxo-1,3-dihydroisobenzofuran-5-carbonitrile.

Referemce:
https://en.wikipedia.org/wiki/Benzofuran,
Benzofuran | C8H6O – PubChem