Heterocyclic Building Block-benzofuran

Study on serum active constituents of rats intragastrically given decoction of fructus psoraleae was written by Song, Dian-rong;Song, Hong-yun;Wang, Yue-fei;Guo, Jie;Xu, Yan-ying;Pan, Gui-xiang. And the article was included in Zhonghua Zhongyiyao Zazhi in 2010.Safety of (Z)-3-(6-(((2S,3R,4S,5S,6R)-3,4,5-Trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)benzofuran-5-yl)acrylic acid This article mentions the following:

Objective: To investigate the active constituents in decoction of Fructus Psoraleae by serum pharmacochem., and illuminate the elemental pharmacodynamic constituents, and provide the foundation for optimizing the prescription of fructus psoraleae. Methods: Based on the establishment of HPLC fingerprint of decoction of Fructus Psoraleae, rat serum were obtained after being given with decoction of Fructus Psoraleae 1 h and 12 h, compared HPLC fingerprints of blank serum, serum containing drug and decoction of Fructus Psoraleae, and the serum active constituents in decoction of Fructus Psoraleae were analyzed. Results: Psoralenoside, isopsoralenoside, psoralen and isopsoralen and the unknown constituent Number3 chromatog. peak were determined in the decoction of Fructus Psoraleae. Psoralenoside, isopsoralenoside, psoralen and isopsoralen were determined in the rat serum after being intragastrically administrated decoction of Fructus Psoraleae 1 h and 12 h. Conclusion: Psoralenoside, isopsoralenoside, psoralen and isopsoralen were the main active constituents and the elemental pharmacodynamic constituents of the decoction of Fructus Psoraleae. In the experiment, the researchers used many compounds, for example, (Z)-3-(6-(((2S,3R,4S,5S,6R)-3,4,5-Trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)benzofuran-5-yl)acrylic acid (cas: 905954-17-8Safety of (Z)-3-(6-(((2S,3R,4S,5S,6R)-3,4,5-Trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)benzofuran-5-yl)acrylic acid).

(Z)-3-(6-(((2S,3R,4S,5S,6R)-3,4,5-Trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)benzofuran-5-yl)acrylic acid (cas: 905954-17-8) belongs to benzofurans derivatives. Benzofuran derivatives have shown many biological activities, including antifungal and antimicrobial properties, and acting as antagonists of H3 receptors and angiotensin II. Substituted benzofurans find applications such as fluorescent sensors, oxidants, in drug discovery, and in another field of chemistry and agriculture.Safety of (Z)-3-(6-(((2S,3R,4S,5S,6R)-3,4,5-Trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)benzofuran-5-yl)acrylic acid

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Halodeboronation of organotrifluoroborates using tetrabutylammonium tribromide or cesium triiodide was written by Yao, Min-Liang;Kabalka, George W.;Blevins, David W.;Reddy, Marepally Srinivasa;Yong, Li. And the article was included in Tetrahedron in 2012.Application of 929626-27-7 This article mentions the following:

Halodeboronation of organotrifluoroborates using com. available tetrabutylammonium tribromide (TBATB) or cesium triiodide in aqueous medium is reported. The mild, transition metal-free method has proven to be tolerant of a wide range of functional groups. High regio- and chemoselectivity are observed Two synthetic routes to (Z)-dibromoalkenes from alkynes, through stereodefined (Z)-2-bromoalkenyltrifluoroborates and (Z)-1,2-bis(boryl)alkenyltrifluoroborates, have been developed using the TBATB mediated bromodeboronation as the key step. In the experiment, the researchers used many compounds, for example, Potassium benzofuran-2-yltrifluoroborate (cas: 929626-27-7Application of 929626-27-7).

Potassium benzofuran-2-yltrifluoroborate (cas: 929626-27-7) belongs to benzofurans derivatives. Benzofuran is the “”parent”” of many related compounds with more complex structures. For example, psoralen is a benzofuran derivative that occurs in several plants. In nature, benzofurans have occupied an important role among the plant phenols & several pharmacologically active compounds.Application of 929626-27-7

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Generation of local redox potential from confined nano-bimetals in porous metal silicate materials for high-performance catalysis was written by Liu, Yang-Yang;Shi, Xiao-Ke;Wu, Chuan-De. And the article was included in Catalysis Science & Technology in 2022.COA of Formula: C8H8O This article mentions the following:

Partial hydrogenation of polycyclic aromatic hydrocarbons (PAHs) could not only produce highly value-added chems. but also reduce environmental pollution; however, the partial hydrogenation reaction has to be performed under extreme conditions in the presence of precious metal-based catalysts, because PAHs are a class of inactive reactants. We report herein a porous metal silicate (PMS) material, PMS-16, that consists of Co and Ni bimetal redox-active species and BIII Lewis acid sites, demonstrating high catalytic activity (>99% conversion) and selectivity (>99%) for hydrogenation of a series of PAHs under mild conditions, which is much superior to noble metal-based catalysts in the literature. The unique catalytic properties of PMS-16 are derived from the synergistic work between Ni and Co metal species by sep. activating different reactant mols. and generating local redox potential to prompt electron and charge transfer. The catalyst is simply produced and very stable for industrial applications. In the experiment, the researchers used many compounds, for example, 2,3-Dihydrobenzo[b]furan (cas: 496-16-2COA of Formula: C8H8O).

2,3-Dihydrobenzo[b]furan (cas: 496-16-2) belongs to benzofurans derivatives. Benzofuran derivatives have shown many biological activities, including antifungal and antimicrobial properties, and acting as antagonists of H3 receptors and angiotensin II. Introduction of benzofurans in organic synthesis, particularly drug synthesis, involves generally the use of their metalated species as nucleophiles in addition reactions or in metal-catalysed cross-coupling reactions.COA of Formula: C8H8O

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Valuable chemicals identified from Flourensia species using vacuum and analytical pyrolysis was written by Silva, Mariana P.;Nieva Lobos, Maria L.;Larson, Tony R.;McQueen-Mason, Simon;Gomez, Leonardo D.;Moyano, E. Laura;Scopel, Ana L.. And the article was included in Journal of Analytical and Applied Pyrolysis in 2022.Related Products of 496-16-2 This article mentions the following:

The genus Flourensia, present throughout most of the Americas has been identified as a source of renewable chems. Here, we characterized the aerial biomass and matrix polysaccharides of Flourensia campestris, F. oolepis and F. riparia, and explored their potential as a source of chems. through the study of two techniques: anal. pyrolysis (PY-GC/MS) and vacuum pyrolysis (VP). In all species, hemicellulose was more abundant than cellulose and lignin, with galacturonic acid being the most abundant monosaccharide. Bio-oils from VP exhibited a complex combination of phenols, terpenes, furans and nitrogen-containing compounds which have a wide range of industrial applications. Differences between the composition of VP pyrolytic oils derived from the mixture of leaves and stems or from individual organs suggest possible interactions between biopolymers. Combining PY-GC/MS and principal component anal. (PCA) we identified fingerprints for leaves and stems of the three Flourensia species. In the experiment, the researchers used many compounds, for example, 2,3-Dihydrobenzo[b]furan (cas: 496-16-2Related Products of 496-16-2).

2,3-Dihydrobenzo[b]furan (cas: 496-16-2) belongs to benzofurans derivatives. Benzofuran derivatives have shown many biological activities, including antifungal and antimicrobial properties, and acting as antagonists of H3 receptors and angiotensin II. Introduction of benzofurans in organic synthesis, particularly drug synthesis, involves generally the use of their metalated species as nucleophiles in addition reactions or in metal-catalysed cross-coupling reactions.Related Products of 496-16-2

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Conjugation of amino-bioactive glasses with 5-aminofluorescein as probe molecule for the development of pH sensitive stimuli-responsive biomaterials was written by Aina, Valentina;Malavasi, Gianluca;Magistris, Claudio;Cerrato, Giuseppina;Martra, Gianmario;Viscardi, Guido;Menabue, Ledi;Lusvardi, Gigliola. And the article was included in Journal of Materials Science: Materials in Medicine in 2014.Reference of 3326-34-9 This article mentions the following:

Bioceramics, such as silica-based glasses, are widely used in bone and teeth restoration. Nowadays, the association between nanotechnol. and pharmacol. is one of the most promising research fields in cancer therapy. The advanced processing methods and new chem. strategies allow the incorporation of drugs within them or on their functionalized surfaces. Bioceramics can act as local drug delivery systems to treat bone and teeth diseases. The present paper reports data related to the development of a pH-stimuli responsive bioactive glass. The glass conjugation with 5-aminofluorescein (5-AF), through a pH-sensitive organic spacer, allows to produce a pH-responsive bioactive biomaterial: when it is exposed to specific pH changes, it can favor the release of 5-AF directly at the target site. 5-AF has been chosen as a simple, low cost, non toxic model to simulate doxorubicin, an anticancer drug. As doxorubicin, 5-AF contains an amino group in its structure to form an amide bond with the carboxylic functionalities of the glass. Raman spectroscopy and thermal anal. confirm the glass conjugation of 5-AF by an amide bond; the amount of 5-AF loaded was very high (≈65 and 44%). The release tests at two different pH (4.2 and 7.4) show that the amount of released 5-AF is higher at acid pH with respect to physiol. one. This preliminary datum evidenced that a pH-sensitive drug delivery system has been developed. The low amount of 5-AF released (<1% of the total 5-AF) is due to the very low solubility of 5-AF in aqueous medium. This disadvantage, may be overcome in a dynamic environment (physiol. conditions), where it is possible to obtain a drug release system ensuring an effective therapeutic dose for long times and, at the same time, avoiding the drug toxicity. In the experiment, the researchers used many compounds, for example, 5-Amino-3′,6′-dihydroxy-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one (cas: 3326-34-9Reference of 3326-34-9).

5-Amino-3′,6′-dihydroxy-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one (cas: 3326-34-9) belongs to benzofurans derivatives. Many natural or synthetic compounds containing benzofuran skeletons have been found to possess remarkable activity as agrochemicals and pharmaceuticals. Benzofurans have also made significant and distinctive contributions to biology. They exhibit several biological activities that range from antiviral, antimicrobial, antitumor, anti-inflammatory.Reference of 3326-34-9

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

A theoretical study of 2-nitrofuran vs 3-nitrofuran as dienophilic electrophile in polar cycloaddition reaction: comparison of the reactivity and reaction mechanism was written by Cainelli, Mauro;Ormachea, Carla M.;Mancini, Pedro M. E.;Kneeteman, Maria N.. And the article was included in International Research Journal of Pure and Applied Chemistry in 2016.Name: Benzofuran-5-ol This article mentions the following:

In this study, we analyzed in a theor. form the behavior of 2-nitrofuran and 3-nitrofuran acting as dienophilic electrophiles in polar cycloaddition reactions joint to different dienes. The reactivity and regioselectivity was discussed employing global and local reactivity indexes, resp. The reaction mechanisms of these cycloadditions were compared through the transition state structures and energies calculated In the experiment, the researchers used many compounds, for example, Benzofuran-5-ol (cas: 13196-10-6Name: Benzofuran-5-ol).

Benzofuran-5-ol (cas: 13196-10-6) belongs to benzofurans derivatives. Benzofurans are only weakly aromatic in nature and they are cleaved by many oxidative and reductive conditions. Benzofurans are stable towards alkali and readily polymerize on treatment with sulfuric acid, due to which they are useful for the preparation of low cost chemically relatively inert resins.Name: Benzofuran-5-ol

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Dextran-based fluorescent nanoprobes for sentinel lymph node mapping was written by Dai, Tingting;Zhou, Shuyan;Yin, Chuyang;Li, Shengli;Cao, Weigang;Liu, Wei;Sun, Kang;Dou, Hongjing;Cao, Yilin;Zhou, Guangdong. And the article was included in Biomaterials in 2014.Formula: C20H13NO5 This article mentions the following:

Biopsy of sentinel lymph node (SLN) has become a common practice to predict whether tumor metastasis has occurred, so proper SLN positioning tracers are highly required. Due to many drawbacks of SLN tracers currently used, developing ideal, biosafe SLN imaging agents is always an urgent issue. The current study designed a novel fluorescent nanoprobe for accurate SLN mapping. Dextran-based nanogel (DNG) was prepared through a highly efficient self-assembly assisted approach and serves as a multi-functional platform for conjugating wide spectra emitting fluorescent agents. The newly fabricated fluorescent DNG (FDNG) could be designed with optimum size and stable fluorescent intensity for specific SLN imaging. Furthermore, a long-term dynamic course in vivo (from 1 min to 72 h) revealed the satisfactory specificity, sensitivity, and stability for SLN mapping. Most importantly, both in vitro and in vivo evaluations indicated that FDNG had fine biosafety and biocompatibility with lymphatic endothelial cells. All these results supported that FDNG could be used as highly efficient mol. imaging probes for specific, sensitive, stable, non-invasive, and safe SLN mapping, which provides efficient and accurate location for SLN biopsy and thus predicts tumor metastasis as well as directs therapies. Besides, our recent studies further demonstrated that DNG could also serve as a specific and controllable drug carrier, indicating a potential application for specific therapies of various lymph-associated diseases. In the experiment, the researchers used many compounds, for example, 5-Amino-3′,6′-dihydroxy-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one (cas: 3326-34-9Formula: C20H13NO5).

5-Amino-3′,6′-dihydroxy-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one (cas: 3326-34-9) belongs to benzofurans derivatives. Benzofurans are compounds with a planar structure having 10 pi electrons that include the lone pair on oxygen atom, which makes it more susceptible to electrophilic attack. As benzofurans are prone to undergo ring opening of the heterocycle, examples of reduction of this type of aromatics by using dissolving metals are rather scarce.Formula: C20H13NO5

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

The synthesis and transition temperatures of 5-(4-alkyl- and 4-alkoxy-phenyl)-2-cyanobenzo[b]furans and a 5-(4′-alkylbiphenyl-4-yl)-2-cyanobenzo[b]furan: a comparison with their biphenyl and terphenyl analogues was written by Friedman, Mark R.;Toyne, Kenneth J.;Goodby, John W.;Hird, Michael. And the article was included in Liquid Crystals in 2001.Synthetic Route of C9H5BrO3 This article mentions the following:

The synthesis and transition temperatures of 5-(4-alkyl- and 4-alkoxy-phenyl)-2-cyanobenzo[b]furans and a 5-(4′-alkylbiphenyl-4-yl)-2-cyanobenzo[b]furan are presented. The 2-cyanobenzo[b]furans show similar mesophase types to the analogous biphenyl and terphenyl compounds, which were obtained by replacing the benzo[b]furan unit with a Ph ring. The transition temperatures for the 2-cyanobenzo[b]furan compounds are always higher than for their biphenyl and terphenyl counterparts, but they are much lower than for the corresponding phenylnaphthalenes. Five mesogenic benzo[b]furans without a cyano group were prepared as intermediates and these compounds have lower clearing points than their biphenyl analogs. In the experiment, the researchers used many compounds, for example, 5-Bromobenzofuran-2-carboxylic acid (cas: 10242-11-2Synthetic Route of C9H5BrO3).

5-Bromobenzofuran-2-carboxylic acid (cas: 10242-11-2) belongs to benzofurans derivatives. Benzofurans are only weakly aromatic in nature and they are cleaved by many oxidative and reductive conditions. Substituted benzofurans find applications such as fluorescent sensors, oxidants, in drug discovery, and in another field of chemistry and agriculture.Synthetic Route of C9H5BrO3

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Multi-small molecule conjugations as new targeted delivery carriers for tumor therapy was written by Shan, Lingling;Liu, Ming;Wu, Chao;Zhao, Liang;Li, Siwen;Xu, Lisheng;Cao, Wengen;Gao, Guizhen;Gu, Yueqing. And the article was included in International Journal of Nanomedicine in 2015.Application of 3326-34-9 This article mentions the following:

In response to the challenges of cancer chemotherapeutics, including poor physicochem. properties, low tumor targeting ability, and harmful side effects, we developed a new tumor-targeted multi-small mol. drug delivery platform. Using paclitaxel (PTX) as a model therapeutic, we prepared two prodrugs, ie, folic acid-fluorescein-5(6)-isothiocyanate-arginine-paclitaxel (FA-FITC-Arg-PTX) and folic acid-5-aminofluorescein-glutamic-paclitaxel (FA-5AF-Glu-PTX), composed of folic acid (FA, target), amino acids (Arg or Glu, linker), and fluorescent dye (fluorescein in vitro or near-IR fluorescent dye in vivo) in order to better understand the mechanism of PTX prodrug targeting. In vitro and acute toxicity studies demonstrated the low toxicity of the prodrug formulations compared with the free drug. In vitro and in vivo studies indicated that folate receptor-mediated uptake of PTX-conjugated multi-small mol. carriers induced high antitumor activity. Notably, compared with free PTX and with PTX-loaded macromol. carriers from our previous study, this multi-small mol.-conjugated strategy improved the water solubility, loading rate, targeting ability, antitumor activity, and toxicity profile of PTX. These results support the use of multi-small mols. as tumor-targeting drug delivery systems. In the experiment, the researchers used many compounds, for example, 5-Amino-3′,6′-dihydroxy-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one (cas: 3326-34-9Application of 3326-34-9).

5-Amino-3′,6′-dihydroxy-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one (cas: 3326-34-9) belongs to benzofurans derivatives. Benzofuran is a core structural unit found in many naturally occurring compounds with multidirectional biological activities. They are also prone to polymerisation in the presence of concentrated mineral acids and Lewis acids.Application of 3326-34-9

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Case Report of COVID-19 Infection After Kidney Transplant Treated With Casirivimab-Imdevimab and Mycophenolate Mofetil Changed to Everolimus was written by Kijima, Yu;Shimizu, Tomokazu;Kato, Shinya;Kano, Kana;Horiuchi, Toshihide;Nozaki, Taiji;Omoto, Kazuya;Inui, Masashi;Toma, Hiroshi;Iida, Shoichi;Takagi, Toshio. And the article was included in Transplantation Proceedings in 2022.SDS of cas: 24280-93-1 This article mentions the following:

Casirivimab-imdevimab is a cocktail of 2 monoclonal antibodies designed to prevent infection by SARS-CoV-2, the virus that causes COVID-19. Casirivimab-imdevimab has been approved in Japan for treating mild to moderate COVID-19; however, to our knowledge, there are no reports of its use after kidney transplant from a live donor. Everolimus, an antineoplastic chemotherapy drug, is expected to be effective in inhibiting the spread of SARS-CoV-2 and preventing its replication, which may facilitate treatment. Here, we report a case of COVID-19 infection after kidney transplant that was initially treated with casirivimab-imdevimab and mycophenolate mofetil but was later changed to everolimus. A 47-yr-old man underwent living donor kidney transplant from his mother in 2017. Immunosuppression therapy was underway through the administration of tacrolimus, mycophenolate mofetil, and methylprednisolone. In early Sept. 2021, he was diagnosed as having COVID-19 and was hospitalized on day 3. On hospitalization, mycophenolate mofetil was discontinued and casirivimab-imdevimab and heparin were started. The patient started an everolimus regimen on day 5. The clin. course was successful without rejection. There was no exacerbation of COVID-19; the patient’s serum creatinine levels and renal function had otherwise remained stable. We could safely treat a patient with casirivimab-imdevimab after kidney transplant. It is suggested that casirivimab-imdevimab can prevent COVID-19 from becoming severe and can be administered without worsening renal function. In addition, everolimus may have inhibited the spread of the virus and prevented it from replicating. In the experiment, the researchers used many compounds, for example, (E)-6-(4-Hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methylhex-4-enoic acid (cas: 24280-93-1SDS of cas: 24280-93-1).

(E)-6-(4-Hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methylhex-4-enoic acid (cas: 24280-93-1) belongs to benzofurans derivatives. Benzofurans are compounds with a planar structure having 10 pi electrons that include the lone pair on oxygen atom, which makes it more susceptible to electrophilic attack. As benzofurans are prone to undergo ring opening of the heterocycle, examples of reduction of this type of aromatics by using dissolving metals are rather scarce.SDS of cas: 24280-93-1

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem