The largest database of trusted experimental protocols

Benzofurans

Benzofurans are a class of aromatic heterocyclic compounds containing a benzene ring fused to a furan ring.
These compounds exhibit a wide range of biological activities and have applications in pharmaceuticals, agrochemicals, and material sciences.
The PubCompare.ai platform leverages AI-driven protocols to optimize Benzofurans research, enabling users to easily locate and compare protocols from literature, pre-prints, and patents to identify the most reproducible and accurate results.
By navigating the vast landscape of Benzofurans research, PubCompare.ai's AI-powered comparisons help researchers find the best protocols and products for their needs, streamlining and enhancing the effciency of their Benzofurans research efforts.

Most cited protocols related to «Benzofurans»

Direct inhibition of thrombin by sulfated benzofuran derivatives was measured through a chromogenic substrate hydrolysis assay.18 (link),19 (link) The buffer used in these experiments was 20 mM Tris-HCl buffer, pH 7.4, containing 100 mM NaCl, 2.5 mM CaCl2, and 0.1% polyethylene glycol (PEG) 8000. Benzofuran derivatives (2 to 30 μL) at concentrations ranging from 4 μg/ml to 5 mg/ml were diluted with appropriate volume of assay buffer in PEG 20,000-coated acrylic cuvettes at 25 °C. To this solution was added 5 μL of thrombin solution to give approximately 5 nM initial thrombin concentration. After 10 min of incubation, 20 μL of 1 mM Spectrozyme TH was rapidly added and the residual thrombin activity was measured from the initial rate of increase in absorbance at 405 nm. Relative residual thrombin activity at each concentration of the inhibitor was calculated from the ratio of thrombin activity in the presence and absence of inhibitor. Logistic equation 1 was used to fit the dose-dependence of residual proteinase activity to obtain the IC50 and the efficacy ΔY (= YM – Y0) of inhibition.
In this equation, Y is the ratio of residual thrombin activity in the presence of inhibitor to that in its absence (fractional residual activity), YM and YO are the maximum and minimum possible values of the fractional residual proteinase activity, IC50 is the concentration of the inhibitor that results in 50% inhibition of enzyme activity, and HS is the Hill Slope, which was set constant at 1. A current version of SigmaPlot (SPSS, Inc. Chicago, IL) was used to perform non-linear curve fitting in which YM, YO and IC50 were allowed to float.
Publication 2011
Benzofurans Biological Assay Buffers Chromogenic Substrates derivatives Endopeptidases enzyme activity Hydrolysis polyethylene glycol 8000 Polyethylene Glycols Psychological Inhibition Sodium Chloride Spectrozyme-TH Thrombin Tromethamine
Method A: Ultrasound-assisted method [30 (link)]. The substituted S-alkylated oxadiazole- and triazole-based benzofuran derivatives were afforded by dissolving 5-(benzofuran-2-yl)-1,3,4-oxadiazole-2-thiol 3 (0.03 g, 0.137 mmol) and 5-(benzofuran-2-yl)-4-phenyl-4H-1,2,4-triazole-3-thiol 6 (0.03 g, 0.103 mmol) inacetonitrile (15 mL). Pyridine (0.213 mmol) was added, and the reaction mixture was stirred for 15 min at 0 °C. The substituted bromoacetanilides 4ag (0.24 mmol) were added, and the reaction mixture was sonicated at 40 °C for 30 min, as shown in Scheme 1. The reaction was monitored viathin-layer chromatography. On completion of the reaction, petroleum ether was added to the mixture with continuous stirring to obtain the final products in the form of precipitates, which were filtered, washed with distilled water and purified.
Method B: Microwave-assisted method [31 (link),32 (link),33 (link)]. Benzofuran–oxadiazole hybrid 3 (0.03 g, 0.137 mmol) and 5-(benzofuran-2-yl)-4-phenyl-4H-1,2,4-triazole-3-thiol 6 (0.03 g, 0.103 mmol) were dissolved in DMF (25 mL). Pyridine (0.213 mmol) was added to the reaction mixtureand stirred for 15 min at 0 °C. The substituted bromoacetanilide derivatives 4ag (0.24 mmol) werethen added, and the reaction mixture was irradiated in a microwave oven for 60–70s, respectively, as depicted in Scheme 1. After completion of the reaction, petroleum ether was added to the reaction mixture with continuous stirring to obtain the final products in the form of precipitates. The precipitates were filtered, washed with distilled waterand purified by recrystallization.The advantages of these preparatory protocols are simplicity, very short reaction times, generality and the elaboration of substituted benzofuran–oxadiazole and benzofuran–triazole with high to excellent yields compared toconventional synthetic approaches and microwave methods already cited for generally synthetic approaches for oxadiazole and triazole derivatives, and specifically benzofuran–oxadiazole and benzofuran–triazole scaffolds [29 (link),34 (link),35 (link),36 (link),37 (link),38 (link),39 (link)].
Full text: Click here
Publication 2022
Benzofurans bromoacetanilide Chromatography derivatives Hybrids Microwaves naphtha Oxadiazoles pyridine Sulfhydryl Compounds Triazoles Ultrasonography
Thrombin activity in the presence of sulfated benzofuran inhibitors was studied using a chromogenic substrate hydrolysis assay in 20 mM Tris-HCl buffer, pH 7.4, containing 100 mM NaCl, 2.5 mM CaCl2 and 0.1 % PEG8000 in PEG20000-coated acrylic cuvettes. Spectrozyme TH was used as substrate and the residual thrombin activity was quantified, as reported earlier.16 (link) Briefly, a solution of 10 μL of an inhibitor to give 1–900 μM final concentration was diluted with 970 μL of the buffer and 5 μL of thrombin (5 nM final concentration). Following incubation for 10 min, 15 μL of 2 mM Spectrozyme TH was added (30 μM final concentration) and the initial rate of hydrolysis from the linear increase in absorbance at 405 nm as a function of time was rapidly measured. Logistic equation 1 was used to fit the dose-dependence of residual thrombin activity to obtain IC50. In this equation, Y is the ratio of residual thrombin activity in the presence of the inhibitor to that in its absence; YM and Y0 are the maximum and minimum possible values of the residual percentage of thrombin activity, respectively; and IC50 is the concentration of inhibitors that results in 50% inhibition of enzyme activity. Sigmaplot 8.0 (SPSS, Inc. Chicago, IL) was used to perform non-linear curve fitting in which YM, YO, HS (Hill Slope), and IC50 were allowed to float.
Publication 2013
Benzofurans Biological Assay Buffers Chromogenic Substrates enzyme activity Hydrolysis inhibitors polyethylene glycol 8000 Psychological Inhibition Sodium Chloride Spectrozyme-TH Thrombin Tromethamine
The SOAC determination was done following previous procedures [21 (link),39 (link),40 (link)] with slight modifications. Briefly, 0.3 g of frozen flavedo tissue was extracted in 6 mL of cooled ethanol:chloroform:water (50:50:1, v:v:v) using a pre-chilled mortar and pestle on an ice bath with sea sand (PanReac AppliChem, Barcelona, Spain) as an abrasive. Then, the homogenate was centrifuged for 5 min at 4500× g at 4 °C, and the collected supernatant was immediately used for analysis.
To measure the extracts 1O2 quenching capacity a competition reaction was carried out using endoperoxide (EP, Invitrotech, Kyoto, Japan) as a singlet oxygen generator and 2,5-diphenyl- 3,4-benzofuran (DPBF, Sigma–Aldrich, Barcelona, Spain) as an UV-Vis absorption probe in a 96-well quartz glass microplate. In each well, 15 µL of the peel extract was mixed with 150 µL of DPBF (0.8 mM solution) and 75 µL of EP (1 mM). The microplate was loaded in dim light and on an ice bath. Absorbance changes of DPBF at 413 nm were monitored during a 90 min reaction at 35 °C using a UV-Vis spectrophotometer microplate reader (SPECTROstar® Omega, BMG Labtech, Offenburg, Germany). α-tocopherol (Sigma–Aldrich, Barcelona, Spain) was used as a standard compound and ethanol:chloroform:water (50:50:1, v:v:v) as a blank. The relative SOAC value for each sample was calculated with the following Formula (2):
Each sample was replicated in 3 wells, and the assay was replicated twice. Results were the mean of the replicates in the 2 microplates (mean ± SE).
Full text: Click here
Publication 2020
alpha-Tocopherol Bath Benzofurans Biological Assay Chloroform diphenyl Ethanol Freezing Light Quartz Singlet Oxygen Tissues
Two sets of ligands were used. The first, illustrated in Figure 3, consisted of 80 CDK2 inhibitors, ranging in pKi from 4.0–8.3. These were split randomly into a training set of 30 and testing set of 50 inhibitors. All molecules were N2, O6 substituted guanines and were the subject of a recent modeling study [2 (link)]. In addition, for some model-building, staurosporine was also used (structure shown in Figure 1), in order to yield a more accurate representation of the absolute configuration of the ligands when bound to CDK2. In these cases, the activity of staurosporine was specified as being greater than a pKi of 7.0. In addition, a set of 67 PDB co-crystal structures of CDK2 bound to non-covalent inhibitors was identified from Binding MOAD [22 (link)] and were mutually aligned in order to provide a direct comparison between QMOD-generated models and the actual CDK2 binding site under normal conformation variation.
The second set, illustrated in Figure 4, consisted of all furan-based quinuclidinene muscarinic antagonists from two structure-activity studies, with the addition of two benzofuran compounds for testing non-additive predictions [20 (link); 21 (link)]. The activity range was pKd 5.0–8.0. These compounds were synthesized as part of an effort to produce a new muscarinic antagonist with reduced dry-mouth side-effects that resulted in the drug tolterodine [23 (link)]. To simulate a typical drug discovery effort focused on a single scaffold (here the furan-based antagonists), models were constructed using known, potent ligands (competitive scaffolds) along with 22 from the furan series. At the time, oxybutynin was a competing therapeutic, atropine was one of the earliest known muscarinic antagonists, and azatadine offered a relatively rigid example of a potent (but non-selective) muscarinic antagonist. The three substituted furans shown at the bottom of Figure 2 were used to test the final model. Of note, the 3-phenyl was the most potent of the series, and (as discussed above) the phenyl-substituted benzofuran was much less active than one would expect based on the activity of the other two test compounds. The split of 22 training and 3 testing ligands was done specifically to illustrate the potential for accurate predictions of highly non-additive effects that depend on molecular alignment.
All ligand structures as well as preparation protocols are available for download (see http://www.jainlab.org for details). Additional details regarding computational procedures for training ligand alignment, model induction, and testing of novel ligands follows.
Publication 2010
antagonists Atropine azatadine Benzofurans Binding Sites CDK2 protein, human furan Furans Guanine inhibitors Ligands Muscarinic Antagonists Muscle Rigidity oxybutynin Pharmaceutical Preparations Staurosporine Therapeutics Tolterodine Xerostomia

Most recents protocols related to «Benzofurans»

Example 162

[Figure (not displayed)]

This compound was synthesized using 5-(8-methoxy-7-quinolyl)spiro[3H-benzofuran-2,4′-piperidine] 2HCl and trimethylsilyl isocyanate. Analysis: LCMS m/z=390 (M+1); 1H NMR (400 MHz, DMSO-d6) δ: 8.94 (dd, J=4.0, 1.8 Hz, 1H), 8.38 (dd, J=8.3, 1.8 Hz, 1H), 7.75 (d, J=8.8 Hz, 1H), 7.59-7.52 (m, 2H), 7.47 (d, J=1.5 Hz, 1H), 7.38 (dd, J=8.3, 1.8 Hz, 1H), 6.88 (d, J=8.3 Hz, 1H), 6.01 (s, 2H), 3.91 (s, 3H), 3.56-3.37 (m, 4H), 3.12 (s, 2H), 1.86-1.64 (m, 4H).

Full text: Click here
Patent 2024
1H NMR Benzofurans Isocyanates Laser Capture Microdissection piperidine Sulfoxide, Dimethyl

Example 157

[Figure (not displayed)]

This compound was synthesized using O-methylhydroxylamine HCl, CDI and 5-(4-methyl-3-quinolyl)spiro[3H-benzofuran-2,4′-piperidine] 2HCl. Analysis: LCMS m/z=404 (M+1); 1H NMR (400 MHz, DMSO-d6) δ: 9.79 (s, 1H), 8.71 (s, 1H), 8.18 (dd, J=8.5, 1.0 Hz, 1H), 8.03 (dd, J=8.3, 1.0 Hz, 1H), 7.81-7.72 (m, 1H), 7.71-7.64 (m, 1H), 7.32 (d, J=1.5 Hz, 1H), 7.19 (dd, J=8.0, 2.0 Hz, 1H), 6.91 (d, J=8.3 Hz, 1H), 3.55 (s, 3H), 3.52-3.43 (m, 2H), 3.41-3.35 (m, 2H), 3.12 (s, 2H), 2.62 (s, 3H), 1.87-1.70 (m, 4H).

Full text: Click here
Patent 2024
1H NMR Benzofurans Lincomycin methoxyamine piperidine Sulfoxide, Dimethyl

Example 152

[Figure (not displayed)]

This compound was synthesized using trimethylsilyl isocyanate and 5-(8-methyl-7-quinolyl)-spiro[3H-benzofuran-2,4′-piperidine] 2HCl. Analysis: LCMS m/z=374 (M+1); 1H NMR (400 MHz, DMSO-d6) δ: 8.96 (dd, J=4.1, 1.9 Hz, 1H), 8.36 (dd, J=8.2, 1.9 Hz, 1H), 7.84 (d, J=8.3 Hz, 1H), 7.54 (dd, J=8.3, 4.3 Hz, 1H), 7.46 (d, J=8.5 Hz, 1H), 7.28 (d, J=1.5 Hz, 1H), 7.16 (dd, J=8.0, 2.0 Hz, 1H), 6.88 (d, J=8.3 Hz, 1H), 6.01 (s, 2H), 3.54-3.36 (m, 4H), 3.12 (s, 2H), 2.68 (s, 3H), 1.86-1.65 (m, 4H).

Full text: Click here
Patent 2024
1H NMR Benzofurans Isocyanates Lincomycin piperidine Sulfoxide, Dimethyl

Example 167

[Figure (not displayed)]

This compound was synthesized using 5-(8-methoxy-7-quinolyl)spiro[3H-benzofuran-2,4′-piperidine] 2HCl and ethoxyamine HCl. Analysis: LCMS m/z=434 (M+1); 1H NMR (400 MHz, DMSO-d6) δ: 9.70 (s, 1H), 8.94 (dd, J=4.3, 1.8 Hz, 1H), 8.38 (dd, J=8.3, 1.8 Hz, 1H), 7.75 (d, J=8.8 Hz, 1H), 7.57 (d, J=8.3 Hz, 1H), 7.54 (dd, J=8.3, 4.3 Hz, 1H), 7.47 (d, J=1.3 Hz, 1H), 7.38 (dd, J=8.3, 2.0 Hz, 1H), 6.88 (d, J=8.3 Hz, 1H), 3.91 (s, 3H), 3.76 (q, J=6.9 Hz, 2H), 3.53-3.42 (m, 2H), 3.40-3.33 (m, 2H), 3.12 (s, 2H), 1.86-1.69 (m, 4H), 1.13 (t, J=7.0 Hz, 3H).

Full text: Click here
Patent 2024
1H NMR Benzofurans Lincomycin piperidine Sulfoxide, Dimethyl

Example 166

[Figure (not displayed)]

This compound was synthesized using 5-(8-methoxy-7-quinolyl)spiro[3H-benzofuran-2,4′-piperidine] 2HCl and O-methylhydroxylamine HCl Analysis: LCMS m/z=420 (M+1); 1H NMR (400 MHz, DMSO-d6) δ: 9.79 (s, 1H), 8.94 (dd, J=4.1, 1.6 Hz, 1H), 8.38 (dd, J=8.3, 1.8 Hz, 1H), 7.75 (d, J=8.8 Hz, 1H), 7.57 (d, J=8.3 Hz, 1H), 7.54 (dd, J=8.3, 4.3 Hz, 1H), 7.47 (d, J=1.3 Hz, 1H), 7.38 (dd, J=8.3, 2.0 Hz, 1H), 6.88 (d, J=8.3 Hz, 1H), 3.91 (s, 3H), 3.55 (s, 3H), 3.52-3.42 (m, 2H), 3.41-3.34 (m, 2H), 3.12 (s, 2H), 1.88-1.66 (m, 4H).

Full text: Click here
Patent 2024
1H NMR Benzofurans Lincomycin methoxyamine piperidine Sulfoxide, Dimethyl

Top products related to «Benzofurans»

Sourced in United States, Germany, United Kingdom, China, Italy, Sao Tome and Principe, France, Macao, India, Canada, Switzerland, Japan, Australia, Spain, Poland, Belgium, Brazil, Czechia, Portugal, Austria, Denmark, Israel, Sweden, Ireland, Hungary, Mexico, Netherlands, Singapore, Indonesia, Slovakia, Cameroon, Norway, Thailand, Chile, Finland, Malaysia, Latvia, New Zealand, Hong Kong, Pakistan, Uruguay, Bangladesh
DMSO is a versatile organic solvent commonly used in laboratory settings. It has a high boiling point, low viscosity, and the ability to dissolve a wide range of polar and non-polar compounds. DMSO's core function is as a solvent, allowing for the effective dissolution and handling of various chemical substances during research and experimentation.
The 12 g column is a laboratory equipment used for chromatographic separation and purification of chemical compounds. It provides a standard size and capacity for conducting various separation techniques. The core function of the 12 g column is to facilitate the efficient separation and isolation of target analytes from complex mixtures.
Silibinin A is a pure compound isolated from the seeds of the milk thistle plant (Silybum marianum). It is used as a reference standard in analytical and research applications.
Silibinin B is a laboratory product manufactured by Merck Group. It is a purified compound derived from the milk thistle plant. Silibinin B is a chemical reference standard used for identification and quantification purposes in analytical procedures.
Sourced in United States, United Kingdom, Germany, Japan, France, Canada
The SpectraMax M2e is a multi-mode microplate reader that can perform absorbance, fluorescence, and luminescence measurements. It is designed for a wide range of applications in life science research and drug discovery.
Sourced in United States
Acetoxymethyl 2-[5-[bis[(acetoxymethoxy-oxo-methyl)methyl]amino]-4-[2-[2-[bis[(acetoxymethoxy-oxo-methyl)methyl]amino]-5-methyl-phenoxy]ethoxy]benzofuran-2-yl]oxazole-5-carboxylate (Fura2-AM) is a fluorescent calcium indicator compound used for measuring intracellular calcium concentrations.
The Small-Molecule Drug Discovery Suite 2018-4 is a comprehensive set of software tools and computational methods developed by Schrödinger for small-molecule drug discovery. The suite includes a range of functionalities for molecular modeling, simulation, and analysis to support the drug discovery process.
Sourced in United States, Germany, United Kingdom, China, Italy, Japan, France, Sao Tome and Principe, Macao, Canada, Spain, India, Belgium, Australia, Israel, Switzerland, Poland, Ireland, Argentina, Austria, Brazil, Sweden, Portugal, New Zealand, Netherlands, Slovakia, Norway, Hungary, Czechia, Denmark
Propidium iodide is a fluorescent dye commonly used in molecular biology and flow cytometry applications. It binds to DNA and is used to stain cell nuclei, allowing for the identification and quantification of cells in various stages of the cell cycle.
Sourced in United States
The XBridge C8 is a high-performance liquid chromatography (HPLC) column designed for the separation and analysis of a wide range of analytes. The column features a silica-based stationary phase with octyl (C8) functionality, providing a balance of hydrophobic and polar interactions for effective separation.
Sourced in United States, Germany, Finland, United Kingdom, Canada, China
The Agilent 7890A is a gas chromatograph designed for the analysis of volatile organic compounds. It features a modular design, temperature-controlled oven, and multi-channel detector options for efficient and reliable separations and quantification.

More about "Benzofurans"

Benzofurans are a class of aromatic heterocyclic compounds that contain a benzene ring fused to a furan ring.
These versatile molecules exhibit a wide range of biological activities and have applications in various fields, including pharmaceuticals, agrochemicals, and material sciences.
Benzofurans are related to other furan-containing compounds, such as DMSO (Dimethyl Sulfoxide), which is a widely used solvent in chemical research.
The 12 g column, a common laboratory tool, can be used for the purification of benzofuran derivatives.
Some notable benzofuran compounds include Silibinin A and Silibinin B, which are known for their potential therapeutic properties.
The SpectraMax M2e is an analytical instrument that can be used to study the spectral characteristics of benzofuran compounds.
Another benzofuran derivative is Acetoxymethyl 2-[5-[bis[(acetoxymethoxy-oxo-methyl)methyl]amino]-4-[2-[2-[bis[(acetoxymethoxy-oxo-methyl)methyl]amino]-5-methyl-phenoxy]ethoxy]benzofuran-2-yl]oxazole-5-carboxylate, also known as Fura2-AM, which is a fluorescent indicator used in calcium imaging studies.
The Small-Molecule Drug Discovery Suite 2018-4 is a comprehensive database that contains information on various small-molecule compounds, including benzofurans, and can be useful for drug discovery research.
Propidium iodide, a fluorescent dye, is commonly used in combination with benzofuran compounds for various applications, such as cell viability assays.
The XBridge C8 is a chromatographic column that can be used for the separation and analysis of benzofuran derivatives.
The Agilent 7890A is a gas chromatography system that can be utilized for the identification and quantification of benzofuran compounds in complex mixtures.
By leveraging the power of AI-driven protocols, the PubCompare.ai platform helps researchers optimize their benzofuran research, enabling them to easily locate and compare protocols from literature, pre-prints, and patents to identify the most reproducible and accurate results.
This streamlines and enhances the effciecy of benzofuran research efforts, allowing researchers to navigate the vast landscape of this diverse class of compounds more effectively.