Day: January 30, 2023

Synthesis of some benzofuro[3,2-d]pyrimidine derivatives as antibacterial and antifungal agents was written by Sangapure, S. S.;Veeresh, D. H.;Yadav, Bodke. And the article was included in Indian Journal of Heterocyclic Chemistry in 2000.Application In Synthesis of 3-Aminobenzofuran-2-carboxamide This article mentions the following:

Condensation of 3-amino-2-benzofurancarboxamide with aromatic aldehydes in presence of catalytic amount of conc hydrochloric acid gave 2-aryl-3,4-dihydro-4-oxobenzofuro[3,2-d]pyrimidines in a single step. Some 2,4-disubstituted benzofuro[3,2-d]pyrimidines have been synthesized. Benzofuropyrimidine derivatives have been screened for antibacterial and antifungal activity against S. aureus, E. coli and C. albicans. In the experiment, the researchers used many compounds, for example, 3-Aminobenzofuran-2-carboxamide (cas: 54802-10-7Application In Synthesis of 3-Aminobenzofuran-2-carboxamide).

3-Aminobenzofuran-2-carboxamide (cas: 54802-10-7) belongs to benzofurans derivatives. Many natural or synthetic compounds containing benzofuran skeletons have been found to possess remarkable activity as agrochemicals and pharmaceuticals. In nature, benzofurans have occupied an important role among the plant phenols & several pharmacologically active compounds.Application In Synthesis of 3-Aminobenzofuran-2-carboxamide

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Structural Analysis and Aggregation Propensity of Reduced and Nonreduced Glycated Insulin Adducts was written by Alavi, Parnian;Yousefi, Reza;Amirghofran, Sara;Karbalaei-Heidari, Hamid Reza;Moosavi-Movahedi, Ali Akbar. And the article was included in Applied Biochemistry and Biotechnology in 2013.Category: benzofurans This article mentions the following:

The milieu within pancreatic β cells represents a favorable environment for glycation of insulin. Therefore, in this study, insulin samples were individually subjected to glycation under reducing and nonreducing conditions. As monitored by ortho-phthalaldehyde and fluorescamine assays, the reduced glycated insulin adduct demonstrates extensively higher level of glycation than the nonreduced glycated counterpart. Also, gel electrophoresis experiments suggest a significant impact of glycation under a reducing system on the level of insulin oligomerization. Furthermore, reduced and nonreduced glycated insulin adducts resp. exhibit full and partial resistance against dithiothreitol-induced aggregation. The results of thioflavin T and Congo red assays suggest the existence of a significant quantity of amyloid-like entities in the sample of reduced glycated insulin adduct. Both fluorescence and far-UV CD studies resp. suggest that the extents of unfolding and secondary structural alteration were closely correlated to the level of insulin glycation. Moreover, the surface tension of two glycated insulin adducts was inversely correlated to their glycation extents and to the quantity of exposed hydrophobic patches. Overall, the glucose-modified insulin mols. under reducing and nonreducing systems display different structural features having significant consequences on aggregation behaviors and surface tension properties. The particular structural constraints of glycated insulin may reduce the binding interaction of this hormone to its receptor which is important for both insulin function and clearance. In the experiment, the researchers used many compounds, for example, 4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione (cas: 38183-12-9Category: benzofurans).

4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione (cas: 38183-12-9) belongs to benzofurans derivatives. Benzofuran is a core structural unit found in many naturally occurring compounds with multidirectional biological activities. Benzofurans have also made significant and distinctive contributions to biology. They exhibit several biological activities that range from antioxidant, antitubercular, antiplasmodial, insecticidal.Category: benzofurans

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Trans-Anethole Abrogates Cell Proliferation and Induces Apoptosis through the Mitochondrial-Mediated Pathway in Human Osteosarcoma Cells was written by Pandit, Kritika;Kaur, Sandeep;Kumar, Ajay;Bhardwaj, Renu;Kaur, Satwinderjeet. And the article was included in Nutrition and Cancer in 2021.COA of Formula: C20H10Cl2O5 This article mentions the following:

Trans-Anethole, the major bioactive component of Illicium verum Hook. commonly known as star anise exhibits various pharmacol. activities including anti-inflammatory, antimicrobial, insecticidal, and antitumor. Osteosarcoma is an extremely aggressive malignant bone tumor that affects children and young adults and accounts for around 60% of all sarcomas. The study was planned to evaluate the potential of trans-Anethole against Human osteosarcoma cell line MG-63. The antiproliferative activity of trans-Anethole was assessed by MTT assay. trans-Anethole exhibited apoptotic cell death as monitored by confocal/electron microscopy and flow cytometry studies. Modulation of gene expression was studied by Western blot and RT-PCR anal. The present study revealed that trans-Anethole inhibited osteosarcoma proliferation in a dose-dependent manner with a GI50 value of 60.25μM and showed pro-apoptotic activity as analyzed by Annexin V-FITC/PI assay. Flow cytometric anal. revealed that trans-Anethole induced cell cycle arrest at the G0/G1 phase with the generation of reactive oxygen species and reduction in mitochondrial membrane potential (ΔΨm). Immunoblotting results showed the increased expression of caspase-9/-3, p53, and decreased expression of Bcl-xL suggesting the involvement of the p53 and mitochondrial intrinsic pathway. This work provides a rationale that trans-Anethole might be considered as a promising chemotherapeutic/nutraceutical agent for the management of osteosarcoma. Highlightstrans-Anethole inhibited cell growth and caused G0/G1 arrest in Human osteosarcoma MG-63 cell line.trans-Anethole led to the loss of mitochondrial membrane permeability along with ROS generation.trans-Anethole upregulates the expression of p53, Caspase-9/-3, and downregulate Bcl-xL expression. In the experiment, the researchers used many compounds, for example, 2′,7′-Dichloro-3′,6′-dihydroxy-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one (cas: 76-54-0COA of Formula: C20H10Cl2O5).

2′,7′-Dichloro-3′,6′-dihydroxy-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one (cas: 76-54-0) belongs to benzofurans derivatives. Benzofuran derivatives are one of the most important oxygen-containing heterocycles. Benzofurans have also made significant and distinctive contributions to biology. They exhibit several biological activities that range from antiviral, antimicrobial, antitumor, anti-inflammatory.COA of Formula: C20H10Cl2O5

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

The budesonide-hydroxypropyl-beta-cyclodextrin complex attenuates ROS generation, IL-8 release and cell death induced by oxidant and inflammatory stress. Study on A549 and A-THP-1 cells was written by Bayiha, Jules Cesar;Evrard, Brigitte;Cataldo, Didier;De Tullio, Pascal;Mingeot-Leclercq, Marie-Paule. And the article was included in Molecules in 2020.Quality Control of 2′,7′-Dichloro-3′,6′-dihydroxy-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one This article mentions the following:

Synthetic glucocorticoids such as budesonide (BUD) are potent anti-inflammatory drugs commonly used to treat patients suffering from chronic inflammatory diseases. A previous animal study reported a higher anti-inflammatory activity with a 2-hydroxypropyl-β-cyclodextrin (HPβCD)-based formulation of BUD (BUD:HPβCD). This study investigated, on cellular models (A549 and A-THP-1), the effect of BUD:HPβD in comparison with BUD and HPβCD on the effects induced by oxidative and inflammatory stress as well as the role of cholesterol. We demonstrated the protective effect afforded by BUD:HPβCD against cytotoxicity and ROS generation induced by oxidative and inflammatory stress. The effect observed for BUD:HPβCD was comparable to that observed with HPβCD with no major effect of cholesterol content. We also demonstrated (i) the involvement of the canonical mol. pathway including ROS generation, a decrease in PI3K/Akt activation, and decrease in phosphorylated/unphosphorylated HDAC2 in the effect induced by BUD:HPβCD, (ii) the maintenance of IL-8 decrease with BUD:HPβCD, and (iii) the absence of improvement in glucocorticoid insensitivity with BUD:HPβCD in comparison with BUD, in conditions where HDAC2 was inhibited. Resulting from HPβCD antioxidant and anticytotoxic potential and protective capacity against ROS-induced PI3K/Akt signaling and HDAC2 inhibition, BUD:HPβCD might be more beneficial than BUD alone in a context of concomitant oxidative and inflammatory stress. In the experiment, the researchers used many compounds, for example, 2′,7′-Dichloro-3′,6′-dihydroxy-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one (cas: 76-54-0Quality Control of 2′,7′-Dichloro-3′,6′-dihydroxy-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one).

2′,7′-Dichloro-3′,6′-dihydroxy-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one (cas: 76-54-0) 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. In nature, benzofurans have occupied an important role among the plant phenols & several pharmacologically active compounds.Quality Control of 2′,7′-Dichloro-3′,6′-dihydroxy-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Determination of sitagliptin with fluorescamine in tablets and spiked serum samples by spectrofluorimetry and a degradation study was written by Caglar, Sena;Onal, Armagan;Toker, Sidika. And the article was included in Current Pharmaceutical Analysis in 2012.Synthetic Route of C17H10O4 This article mentions the following:

Two novel, simple, and rapid stability-indicating spectrofluorimetric methods were developed for the determination of sitagliptin in tablets and spiked serum samples. In the first method, sitagliptin’s natural fluorescence was measured at 353 nm after excitation at 259 nm. On the basis of the reaction between sitagliptin and fluorescamine the second method was developed in borate buffer solution of pH 9.0 and the fluorescence intensities of the derivatives were measured at 475 nm emission and 390 nm excitation wavelengths. The calibration curves were constructed in concentration range of 0.5-10.0 μg mL^-1 and 0.2-1.4 μg mL^-1 for the first and second method, resp. The developed methods were validated with respect to linearity, precision, sensitivity, accuracy and selectivity. The degradation behavior of the drug was investigated using the first method. The drug solution was subjected to neutral, acid and alkali hydrolysis, oxidation, thermal stress and exposured to the sunlight. The first method is proved to be selective and useful for the investigation of the stability of sitagliptin. The application of spiked serum samples was also analyzed by the second method. The developed methods were successfully applied for the determination of sitagliptin in tablets and spiked serum samples. In the experiment, the researchers used many compounds, for example, 4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione (cas: 38183-12-9Synthetic Route of C17H10O4).

4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione (cas: 38183-12-9) 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. 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.Synthetic Route of C17H10O4

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Biocompatible antimicrobial electrospun nanofibers functionalized with ε-poly-L-lysine was written by Amariei, Georgiana;Kokol, Vanja;Vivod, Vera;Boltes, Karina;Leton, Pedro;Rosal, Roberto. And the article was included in International Journal of Pharmaceutics (Amsterdam, Netherlands) in 2018.Category: benzofurans This article mentions the following:

The antimicrobial polypeptide ε-poly(L-lysine) (ε-PL) was electrostatically incorporated to poly(acrylic acid) (PAA)/poly(vinyl alc.) (PVA) electrospun nanofibers. ε-PL loading and distribution was assessed by IR spectra, ζ-potential measurements and the primary amino reactive dye fluorescamine. Functionalized fibers with 485 ± 140 nm diameter, could be loaded with 0.57-0.74 g ε-PL (g dressing)^-1 that released at a constant rate of 5.4 ± 2.8 mg ε-PL (g dressing day)^-1. Such a dressings resulted in two orders of magnitude lower bacterial colonization than non-functionalized PAA-PVA after 14 days of incubation. Bacterial impairment was attributed to the damage of cell membranes and the formation of intracellular reactive oxygen species. ε-PL functionalized nanofibers did not display cytotoxicity to human corneal epithelial cells, HCEpC, in 24 h MTT assays. However, the viability of rapidly growing tumoral HeLa cells decreased >50% under the same conditions. The prepared biocompatible nanofibrous dressings with durable antibacterial activity show potential application as wound dressings and other biomedical uses. In the experiment, the researchers used many compounds, for example, 4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione (cas: 38183-12-9Category: benzofurans).

4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione (cas: 38183-12-9) belongs to benzofurans derivatives.Benzofuran is one of the most significant oxygen-containing heterocycles consisting of fused benzene and furan ring, which are widely presented in various naturally occurring and synthetically active compounds. They are also prone to polymerisation in the presence of concentrated mineral acids and Lewis acids.Category: benzofurans

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Preparation of benzo[b]furans having five-membered heterocycles at the 2-position and 2-(4-alkylcarbamoylbuta-1,3-dienyl)benzo[b]furans, and their cysteinyl leukotriene receptor (cysLT1, cysLT2) inhibitory activity was written by Akai, Yukiko;Tabuchi, Yukako;Ando, Kumiko;Ito, Azusa;Sakata, Yoko;Kawasaki, Ikuo;Ohishi, Takahiro;Yamashita, Masayuki;Ohta, Shunsaku;Nishide, Kiyoharu;Ohishi, Yoshitaka. And the article was included in Chemical & Pharmaceutical Bulletin in 2012.Formula: C10H7BrO2 This article mentions the following:

A series of benzo[b]furan derivatives having a 5-membered heterocyclic substituent at the 2-position were prepared from 2-(1-chloro-2-formylvinyl)benzo[b]furans and 2-[4-(alkylcarbamoyl)buta-1,3-dienyl]benzo[b]furans. The newly prepared 2-heterocyclic benzo[b]furans were evaluated for their cysteinyl leukotriene receptor (cysLT1, cysLT2) inhibitory activity. Several compounds showed moderate inhibition of Ca mobilization in HEK 293T-cysLT2 or CHO-cysLT1 cells. In the experiment, the researchers used many compounds, for example, 1-(5-Bromobenzofuran-2-yl)ethanone (cas: 38220-75-6Formula: C10H7BrO2).

1-(5-Bromobenzofuran-2-yl)ethanone (cas: 38220-75-6) belongs to benzofurans derivatives. Benzofurans are only weakly aromatic in nature and they are cleaved by many oxidative and reductive conditions. Benzofurans have also made significant and distinctive contributions to biology. They exhibit several biological activities that range from antioxidant, antitubercular, antiplasmodial, insecticidal.Formula: C10H7BrO2

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Structure-in vitro activity relationships of pentamidine analogs and dication-substituted bis-benzimidazoles as new antifungal agents was written by Del Poeta, Maurizio;Schell, Wiley A.;Dykstra, Christine C.;Jones, Susan;Tidwell, Richard R.;Czarny, Agnieszka;Bajic, Miroslav;Bajic, Marina;Kumar, Arvind;Boykin, David;Perfect, John R.. And the article was included in Antimicrobial Agents and Chemotherapy in 1998.Recommanded Product: 1-(5-Bromobenzofuran-2-yl)ethanone This article mentions the following:

Twenty analogs of pentamidine (including I), 7 primary metabolites of pentamidine, and 30 dicationic substituted bisbenzimidazoles were screened for their inhibitory and fungicidal activities against Candida albicans and Cryptococcus neoformans. A majority of the compounds had MICs at which 80% of the strains were inhibited (MIC₈₀s) comparable to those of amphotericin B and fluconazole. Unlike fluconazole, many of these compounds, such as II and III, were found to have potent fungicidal activity. The most potent compound against C. albicans had an MIC₈₀ of ≤0.09 μg/mL, and the most potent compound against C. neoformans had an MIC₈₀ of 0.19 μg/mL. Selected compounds, such as IV, were also found to be active against Aspergillus fumigatus, Fusarium solani, Candida species other than C. albicans, and fluconazole-resistant strains of C. albicans and C. neoformans. It is clear from the data presented here that further studies on the structure-activity relationships, mechanisms of action and toxicities, and in vivo efficacies of these compounds are warranted to determine their clin. potential. In the experiment, the researchers used many compounds, for example, 1-(5-Bromobenzofuran-2-yl)ethanone (cas: 38220-75-6Recommanded Product: 1-(5-Bromobenzofuran-2-yl)ethanone).

1-(5-Bromobenzofuran-2-yl)ethanone (cas: 38220-75-6) belongs to benzofurans derivatives.Benzofuran is one of the most significant oxygen-containing heterocycles consisting of fused benzene and furan ring, which are widely presented in various naturally occurring and synthetically active compounds. They are also prone to polymerisation in the presence of concentrated mineral acids and Lewis acids.Recommanded Product: 1-(5-Bromobenzofuran-2-yl)ethanone

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Morroniside protects OLN-93 cells against H₂O₂-induced injury through the PI3K/Akt pathway-mediated antioxidative stress and antiapoptotic activities was written by Li, Fengzhi;Song, Xue;Xu, Jiaxin;Shi, Yujiao;Hu, Ruina;Ren, Zhen;Qi, Qi;Lu, Hezuo;Cheng, Xiaoxin;Hu, Jianguo. And the article was included in Cell Cycle in 2021.COA of Formula: C20H10Cl2O5 This article mentions the following:

Neurodegenerative disorders, including spinal cord injury (SCI), result in oxidative stress-induced cell damage. Morroniside (MR), a major active ingredient of the Chinese herb Shan Zhu Yu, has been shown to ameliorate oxidative stress and inflammatory response. Our previous study also confirmed that morroniside protects SK-N-SH cell line (human neuroblastoma cells) against oxidative impairment. However, it remains unclear whether MR also plays a protective role for oligodendrocytes that are damaged following SCI. The present study investigated the protective effects of MR against hydrogen peroxide (H₂O₂)-induced cell death in OLN-93 cells. MR protected OLN-93 cells from H₂O₂-induced injury, attenuated H₂O₂-induced increase in reactive oxygen species (ROS) and malondialdehyde (MDA) levels, and blocked the reduction of mitochondrial membrane potential (MMP) induced by H₂O₂. MR enhanced the activity of the antioxidant enzyme superoxide dismutase (SOD) and suppressed H₂O₂-induced downregulation of the antiapoptotic protein Bcl-2 and activation of the proapoptotic protein caspase-3. Finally, we found that LY294002, a specific inhibitor of the PI3K/Akt pathway, inhibited the protective effect of MR against H₂O₂-induced OLN-93 cell injury in the MTT and TUNEL assays. LY294002 also inhibited the expression of SOD and Bcl-2, and increased the expression of iNOS and c-caspase-3 induced by MR treatment. MR exerts protective effects against H₂O₂-induced OLN-93 cell injury through the PI3K/Akt signaling pathway-mediated antioxidative stress and antiapoptotic activities. MR may provide a potential strategy for SCI treatment or other related neurodegeneration. In the experiment, the researchers used many compounds, for example, 2′,7′-Dichloro-3′,6′-dihydroxy-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one (cas: 76-54-0COA of Formula: C20H10Cl2O5).

2′,7′-Dichloro-3′,6′-dihydroxy-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one (cas: 76-54-0) 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.COA of Formula: C20H10Cl2O5

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Borrowing Carbonate-Enabled Allylic Amination Reactions under Additive- and Reductant-Free Nickel Catalysis Employing Allylic Alcohols was written by Vaidya, Gargi Nikhil;Nagpure, Mithilesh;Kumar, Dinesh. And the article was included in ACS Sustainable Chemistry & Engineering in 2021.Product Details of 54802-10-7 This article mentions the following:

“Borrowing carbonate”-enabled allylic cross-amination reactions employing allylic alcs., e.g., cinnamyl alc., (E)-3-(4-methoxyphenyl)prop-1-en-1-ol, and (E)-3-(furan-2-yl)prop-1-en-1-ol, were discovered via merging acyl/allyl C-O bonds activation under nickel catalysis. The key component of this protocol is the ability of nickel [Ni(II)-Ni(0)] to execute a relay process via the nucleophilic trapping of the generated acyl Ni complex, resulting from the acyl C-O bond cleavage of dialkyl carbonates, followed by selective allylic C-O bond activations (allylic C-O vs alkyl C-O vs acyl C-O) to yield π-allyl-Ni-complexes. The finding truly represents Ni-catalyzed green allylic amination reactions under additive(s)-free conditions with excellent chemo- (N vs O), regio- (linear vs branched), and stereoselectivity (E vs Z) with a wide range of fundamentally challenging N-heterocycles, e.g., 2(1H)-pyridone, isoquinolin-1(2H)-one, and benzo[d]thiazol-2(3H)-one, and allylic alcs. The reaction is scalable, does not require harmful reaction media and a globe box, and is successfully applied to the scale-up synthesis of pharmaceuticals (cinnarizine, flunarizine, and naftifine) with promising yields. In the experiment, the researchers used many compounds, for example, 3-Aminobenzofuran-2-carboxamide (cas: 54802-10-7Product Details of 54802-10-7).

3-Aminobenzofuran-2-carboxamide (cas: 54802-10-7) belongs to benzofurans derivatives. Benzofuran derivatives are one of the most important oxygen-containing heterocycles. Benzofurans have also made significant and distinctive contributions to biology. They exhibit several biological activities that range from antiviral, antimicrobial, antitumor, anti-inflammatory.Product Details of 54802-10-7

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem