Category: benzofurans

Novel benzofuran-based sulphonamides as selective carbonic anhydrases IX and XII inhibitors: synthesis and in vitro biological evaluation was written by Abdelrahman, Mohamed A.;Eldehna, Wagdy M.;Nocentini, Alessio;Ibrahim, Hany S.;Almahli, Hadia;Abdel-Aziz, Hatem A.;Abou-Seri, Sahar M.;Supuran, Claudiu T.. And the article was included in Journal of Enzyme Inhibition and Medicinal Chemistry in 2020.Category: benzofurans This article mentions the following:

Pursuing on our efforts toward searching for efficient hCA IX and hCA XII inhibitors, herein we report the design and synthesis of new sets of benzofuran-based sulfonamides, featuring the zinc anchoring benzenesulfonamide moiety linked to a benzofuran tail via a hydrazine or hydrazide linker. All the target benzofurans were examined for their inhibitory activities toward isoforms hCA I, II, IX, and XII. The target tumor-associated hCA IX and XII isoforms were efficiently inhibited with K_Is spanning in ranges 10.0-97.5 and 10.1-71.8 nM, resp. Interestingly, arylsulfonehydrazones displayed the best selectivity toward hCA IX and XII over hCA I (SIs: 39.4-250.3 and 26.0-149.9, resp.), and over hCA II (SIs: 19.6-57.1 and 13.0-34.2, resp.). Furthermore, the target benzofurans were assessed for their anti-proliferative activity, according to US-NCI protocol, toward a panel of sixty cancer cell lines. Only benzofurans and possessed selective and moderate growth inhibitory activity toward certain cancer cell lines. In the experiment, the researchers used many compounds, for example, 1-(5-Bromobenzofuran-2-yl)ethanone (cas: 38220-75-6Category: benzofurans).

1-(5-Bromobenzofuran-2-yl)ethanone (cas: 38220-75-6) 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. Benzofurans have also made significant and distinctive contributions to biology. They exhibit several biological activities that range from antiviral, antimicrobial, antitumor, anti-inflammatory.Category: benzofurans

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Preparation and Properties of Cationic Gelatin Cross-Linked with Tannin was written by Yu, Ning;Li, Junying;Ma, Feng;Yang, Pengfei;Liu, Wenjie;Zhou, Mingyang;Zhu, Zhifei;Xing, Shu. And the article was included in Journal of Agricultural and Food Chemistry in 2020.Reference of 38183-12-9 This article mentions the following:

A kind of biomaterial with antibacterial and mech. properties was prepared using gelatin (GE) as a raw material. GE was modified by antibacterial epoxy quaternary ammonium salt (QAS) and then crosslinked with tannic acid (TA). Anal. of the Fourier transform IR spectroscopy (FTIR) results showed that the cationic group was grafted onto GE by reaction of the amino of GE with the epoxy of QAS, and the crosslinking occurred between the amino of GE and the active groups of TA under alk. conditions. The crosslinking degree was determined by the fluorescence method via a derivative reaction of fluorescamin. The influence of the crosslinking degree on the phys. and chem. properties of the GE film was studied by SEM, differential scanning calorimetry (DSC), thermogravimetric anal. (TGA), X-ray diffraction (XRD), and mech. testing. The results showed that the modified GE film formed a compact crosslinking structure, and its thermostability and mech. properties were improved with increasing crosslinking degree. The in vitro antibacterial rate of the crosslinked cationic GE film to Escherichia coli (E. coli) and Staphylococcus aureus (S. aureus) reached 95.83% and 100% resp., and the in vitro cell relative growth rate (RGR) of HeLa cells cultured in the extracted leachate of the crosslinked cationic GE film exceeded 85%, which illustrated that the modified GE film had excellent antibacterial activity and biocompatibility. In the experiment, the researchers used many compounds, for example, 4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione (cas: 38183-12-9Reference of 38183-12-9).

4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione (cas: 38183-12-9) 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 antioxidant, antitubercular, antiplasmodial, insecticidal.Reference of 38183-12-9

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Cholinergic system and exploratory behavior are changed after weekly-binge ethanol exposure in zebrafish was written by Bernardo, Henrique Teza;Agostini, Jotele Fontana;Toe, Helena Cristina Zuehl Dal;Vieira, Karine Medeiros;Baldin, Samira Leila;Schuck, Patricia Fernanda;Uribe-Cruz, Carolina;Longo, Larisse;da Silveira, Themis Reverbel;Rosemberg, Denis Broock;Rico, Eduardo Pacheco. And the article was included in Pharmacology, Biochemistry and Behavior in 2019.Synthetic Route of C20H10Cl2O5 This article mentions the following:

Binge drinking is characterized by excessive alc. consumption in a short period of time and is associated with a poor quality of life. Zebrafish are commonly used to investigate neurochem., behavioral, and genetic parameters associated with ethanol (EtOH) exposure. However, few studies have used zebrafish as a model to investigate binge EtOH exposure. In order to elucidate the potential neurobehavioral impairments evoked by binge EtOH exposure in zebrafish, animals were immersed in 1.4% EtOH for 30 min three consecutive times with intervals of one week. Neurobehavioral parameters were analyzed immediately following the third exposure, as well as 2 and 9 days later. Brain choline acetyltransferase (ChAT) and acetylcholinesterase (AChE) activities were reduced 9 days after the treatment. Thiobarbituric acid-reactive species and dichlorodihydrofluorescein levels were increased immediately after the treatment, but both returned to normal levels 2 days after the treatment. Catalase and glutathione reductase were impaired 2 and 9 days after the treatment. No alteration was observed in superoxide dismutase and glutathione peroxidase activities. EtOH treatment did not alter brain expression of inflammatory genes such as il-1β, il-10, and tnf-α . Zebrafish displayed anxiolytic-like behavior immediately after the last exposure, though there was no behavioral alteration observed 9 days after the treatment. Therefore, binge EtOH exposure in zebrafish leads to long lasting brain cholinergic alteration, probably related to oxidative stress immediately after the exposure, which is independent of classical inflammatory markers. 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: 76-54-0Synthetic Route of C20H10Cl2O5).

2′,7′-Dichloro-3′,6′-dihydroxy-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one (cas: 76-54-0) belongs to benzofurans derivatives. Benzofuran is a core structural unit found in many naturally occurring compounds with multidirectional biological activities. In nature, benzofurans have occupied an important role among the plant phenols & several pharmacologically active compounds.Synthetic Route of C20H10Cl2O5

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Impaction of factors associated with oxidative stress on the pathogenesis of gestational hypertension and preeclampsia: A Chinese patients based study was written by Qiu, Dongmei;Wu, Jufei;Li, Min;Wang, Li;Zhu, Xianggan;Chen, Youguo. And the article was included in Medicine (Philadelphia, PA, United States) in 2021.Synthetic Route of C20H10Cl2O5 This article mentions the following:

We aimed to investigate the effect of Kelch-like ECH-associated protein 1/NF-E2 p45-related factor 2 (Keap1/Nrf2) pathway on the biol. function of trophoblast cells in oxidative stress model at the cellular level, and analyzed the expression level and clin. significance of Keap1/Nrf2 pathway and related antioxidant factors in placental tissues of Preeclampsia (PE) patients at clin. level. In present study, we found that under hypoxia/reoxygenation conditions, the activity of oxidative stress-related enzymes (CAT, GSH-Px, SOD) in HTR8/SVneo cells was significantly lower than that before treatment (P<01). The activities of CAT, GSH-Px and SOD in HTR8/SVneo cells in SiRNA+H/R group decreased significantly (P<01), indicating the important defense effect of Keap1/Nrf2 signaling pathway in oxidative stress. As a control group of Nrf2SiRNA+H/R group, Si-NC+H/R group had CAT, GSH-Px and SOD activities decreasing, which was similar to that in H/R group. Moreover, the activities of oxidative stress-related active enzymes in patients with PE were further confirmed by detecting and comparing the activities of CAT, GSH-Px and SOD in placental tissues. The results showed that the activity of SOD (P<001), GSH-Px (P<01) and CAT (P<01) in placental tissues of patients with PE were significant different from those of normal placental tissues. The expression level of Keap1 in placenta of patients with PE was slightly lower than that of normal placenta. While the expression of Nrf2 in placenta of patients with PE was significantly higher than that of normal placenta. HO-1 expression in placenta of patients with PE was significantly higher than that of normal placenta. These results implicate the importance of Keap-1/Nrf2 pathway in PE. 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: 76-54-0Synthetic Route of 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 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.Synthetic Route of C20H10Cl2O5

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Synthesis, characterisation and antibacterial activities of titanium(III) complexes with schiff bases derived from benzofuran was written by Kannojia, Poonam;Sahdev. And the article was included in Oriental Journal of Chemistry in 2011.COA of Formula: C9H8N2O2 This article mentions the following:

Titanium(III) chloride reacts with Schiff bases derived from benzaldehydes/acetophenone with 3-aminobenzofuran-2-carboxamide/ethyl 3-aminobenzofuran-2-carboxylate to yield complexes having general composition [Ti(L)₂(H₂O)₂]Cl₃ (L = Schiff base). The ligands and their corresponding Ti(III) complexes were characterized by elemental analyses, molar conductance,magnetic susceptibility, IR and electronic spectra and TGA. The ligands act in a bidentate manner. Based on these studies octahedral geometries are proposed for these complexes. The ligands and their Ti(III)complexes have screened for antibacterial activities. In the experiment, the researchers used many compounds, for example, 3-Aminobenzofuran-2-carboxamide (cas: 54802-10-7COA of Formula: C9H8N2O2).

3-Aminobenzofuran-2-carboxamide (cas: 54802-10-7) 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. 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: C9H8N2O2

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Effects of operating conditions on PM oxidative potential assays was written by Frezzini, Maria Agostina;De Francesco, Nayma;Massimi, Lorenzo;Canepari, Silvia. And the article was included in Atmospheric Environment in 2022.Name: 2′,7′-Dichloro-3′,6′-dihydroxy-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one This article mentions the following:

Oxidative potential (OP) has been suggested as a biol. relevant exposure metric for estimating particulate matter (PM) capacity to induce oxidative stress in living organisms. However, standardized exptl. procedures are not yet available. This study explores how a variety of operating conditions influences responses of several different assays for measuring OP: the 2′,7′-dichlorofluorescein (OP^DCFH), the ascorbic acid (OP^AA) and the dithiothreitol (OP^DTT) assays. A recently optimized method for the evaluation of PM reducing properties, based on the 2,2-diphenyl-1-picrylhydrazyl assay (RP^DPPH), was also included in the study. Two monitoring campaigns were carried out in Central Italy by using co-located PM10 samplers working in parallel, for comparing results obtained from different operating procedures simultaneously applied on equivalent samples. Extraction efficiency and repeatability of three different water-extraction methods (rotating agitator, ultrasonic bath, and vortex), and the influence of storage duration and conditions on OP results were examined OPDCFH values were found to be significantly higher when ultrasonic bath (US) was used for extraction, probably due to the formation of free radicals induced by US; for all the OP assays, the highest repeatability was obtained by extracting samples with rotating agitator (RA). Sample storage was confirmed to be a very critical issue as all the assays, except OP^DTT, showed a marked dependence on storage time and conditions. The influence of membrane filters used to collect PM was also assessed. No significant differences were observed between samples collected on quartz and polytetrafluoroethylene (PTFE) membrane filters, except for OP^AA, that gave significantly higher results for samples collected on PTFE membranes. Lastly, the contribution of water-insoluble PM components to OP was examined and warrants further investigations. 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: 76-54-0Name: 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. Benzofuran derivatives are one of the most important oxygen-containing heterocycles. They are also prone to polymerisation in the presence of concentrated mineral acids and Lewis acids.Name: 2′,7′-Dichloro-3′,6′-dihydroxy-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Synthesis and antimicrobial activity of some imidazothiazole derivatives of benzofuran was written by Shankerrao, Sheelavanth;Bodke, Yadav D.;Santoshkumar, S.. And the article was included in Arabian Journal of Chemistry in 2017.Recommanded Product: 1-(5-Bromobenzofuran-2-yl)ethanone This article mentions the following:

A series of 6-(5-substituted-benzofuran-2-yl)-3-phenylimidazo[2,1-b][1,3]thiazoles I (R¹ = H, Br; R² = H, CH₃, F) and 3,6-bis(5-substituted-benzofuran-2-yl)imidazo[2,1-b][1,3]thiazoles II (R³ = H, Br) was synthesized by the reaction of 1-(1-benzofuran-2-yl)-2-bromoethanones such as 1-(1-benzofuran-2-yl)-2-bromoethanone, 2-bromo-1-(5-bromo-1-benzofuran-2-yl)ethanone with 4-phenyl-1,3-thiazol-2-amines such as 4-phenyl-thiazol-2-ylamine, 4-p-tolyl-thiazol-2-ylamine, 4-(4-fluoro-phenyl)-thiazol-2-ylamine and 4-benzofurano-1,3-thiazol-2-amines such as 4-(1-benzofuran-2-yl)-1,3-thiazol-2-amine, 4-(5-bromo-1-benzofuran-2-yl)-1,3-thiazol-2-amine resp. The structures of newly synthesized compounds I and II were characterized by IR, ¹H NMR and mass spectroscopic studies and screened for their antimicrobial activities. The preliminary results revealed that some of the compounds exhibited promising antimicrobial activities. 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 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 antioxidant, antitubercular, antiplasmodial, insecticidal.Recommanded Product: 1-(5-Bromobenzofuran-2-yl)ethanone

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Photochemical reaction of benzofuran derivatives with benzophenone or benzaldehyde was written by Kawase, Yoshiyuki;Yamaguchi, Seiji;Ochiai, Hirokazu;Horita, Hisanori. And the article was included in Bulletin of the Chemical Society of Japan in 1974.HPLC of Formula: 1646-27-1 This article mentions the following:

Photochem. reaction of the benzofurans I [R = R1 = Me; R = Me, CH2OH, R1 = H; RR1 = (CH2)4] with benzophenone gave the oxetanes II (R2 = Ph). Oxetanes II (R2 = H) were produced by the reaction of I with benzaldehyde, but yields were not so high because of their instability. The reaction of 2-methoxycarbonyl- and 2-cyano-benzofuran with benzophenone or benzaldehyde gave dimers of the benzofurans. In the experiment, the researchers used many compounds, for example, Methyl benzofuran-2-carboxylate (cas: 1646-27-1HPLC of Formula: 1646-27-1).

Methyl benzofuran-2-carboxylate (cas: 1646-27-1) belongs to benzofurans derivatives. Many natural or synthetic compounds containing benzofuran skeletons have been found to possess remarkable activity as agrochemicals and pharmaceuticals. 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.HPLC of Formula: 1646-27-1

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Direct carboxylation of simple arenes with CO₂ through a rhodium-catalyzed C-H bond activation was written by Suga, Takuya;Mizuno, Hajime;Takaya, Jun;Iwasawa, Nobuharu. And the article was included in Chemical Communications (Cambridge, United Kingdom) in 2014.Electric Literature of C10H8O3 This article mentions the following:

Direct carboxylation of simple arenes under atm. pressure of CO₂ is achieved through a rhodium-catalyzed C-H bond activation without the assistance of a directing group. Various arenes such as benzene, toluene, xylene, electron-rich or electron-deficient benzene derivatives, and heteroaromatics are directly carboxylated with high TONs. In the experiment, the researchers used many compounds, for example, Methyl benzofuran-2-carboxylate (cas: 1646-27-1Electric Literature of C10H8O3).

Methyl benzofuran-2-carboxylate (cas: 1646-27-1) 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 antioxidant, antitubercular, antiplasmodial, insecticidal.Electric Literature of C10H8O3

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

A mix-and-click method to measure amyloid-β concentration with sub-micromolar sensitivity was written by Xue, Christine;Lee, Yoon Kyung;Tran, Joyce;Chang, Dennis;Guo, Zhefeng. And the article was included in Royal Society Open Science in 2017.Formula: C17H10O4 This article mentions the following:

Aggregation of amyloid-β (Aβ) protein plays a central role in Alzheimer’s disease. Because protein aggregation is a concentration-dependent process, rigorous investigations require accurate concentration measurements. Owing to the high aggregation propensity of Aβ protein, working solutions of Aβ are typically in the low micromolar range. Therefore, an ideal Aβ quantification method requires high sensitivity without sacrificing speed and accuracy. Absorbance at 280nm is frequently used to measure Aβ concentration, but the sensitivity is low with only one tyrosine and no tryptophan residues in the Aβ sequence. Here we present a fluorescence method for Aβ quantification using fluorescamine, which gives high fluorescence upon reaction with primary amines.We show that, using hen egg white lysozyme as a standard, fluorescence correlates linearly with primary amine concentration across a wide range of fluorescamine concentrations, from 62.5 to 1000μM. The maximal sensitivity of detection is achieved at a fluorescamine concentration of 250μM or higher. The fluorescamine method is compatible with the presence of DMSO, which is commonly used in the preparation of Aβ oligomers, and limits the use of absorbance at 280nm due to its high background reading. Using aggregation kinetics, we show that the fluorescaminemethod gives accurate concentration measurements at low micromolar range and leads to highly consistent aggregation data. We recommend the fluorescamine assay to be used for routine and on-thefly concentration determination in Aβ oligomerization and fibrillization experiments In the experiment, the researchers used many compounds, for example, 4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione (cas: 38183-12-9Formula: C17H10O4).

4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione (cas: 38183-12-9) 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 antioxidant, antitubercular, antiplasmodial, insecticidal.Formula: C17H10O4

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem