Category: benzofurans

In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Kinetics of drug decomposition. Part 38. Hydrolysis and autoxidation of sodium phenylbutazone and aminophenazone in binary kinetic system, published in 1976, which mentions a compound: 129-18-0, Name is Sodium 4-butyl-3,5-dioxo-1,2-diphenylpyrazolidin-4-ide, Molecular C19H19N2NaO2, Reference of Sodium 4-butyl-3,5-dioxo-1,2-diphenylpyrazolidin-4-ide.

The kinetics of hydrolysis and autoxidation of Na phenylbutazone (Na I)(II) [129-18-0] and aminophenazone (III) [58-15-1] in binary sysytems (e.g., Rheumopyrin [8066-94-2] and Irgapyrin [8064-79-7]) was investigated in NH3-AcOH, Carmody and Wefford buffers at different buffer concentration, pH, ionic strengths, and temperature The degradation of II in the presence of III followed 1st order reaction kinetics. III degradation at low concentration (in buffers-Ph 7.13-10.0) was possible only under high excess O. High concentrations of II and III (15%) can be considered as a system stabilizing the degradation, which was regulated by the alk. character of II (pH = 8.6 to 15% II). The lack of effect of different kinds of buffers, ionic strength, and pH on the rate constant of II hydrolysis, qualified the process as a spontaneous reaction initiated by the attack of water mols. The degradation parameters of II in the presence of III, compared with those in its absence, confirm the stabilizing effect of III. In the autoxidation and hydrolysis reaction of II, the changes in the reaction rate depended on the pH. At pH 7.13, the degradation was 3 times faster than at pH 12.07. The activation energy values for the hydrolysis of II without III were lower by 19240 J/mole and for the autoxidation and hydrolysis by 2700 J/mole than those for III present in the reaction medium.

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In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Evaluation of chemical cross-linkers for in-depth structural analysis of G protein-coupled receptors through cross-linking mass spectrometry, published in 2020-03-15, which mentions a compound: 70539-42-3, Name is Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, Molecular C18H20N2O12, Related Products of 70539-42-3.

Chem. crosslinking would conceivably cause structural disruption of a protein, but few cross-linkers have been fully evaluated in this aspect. Furthermore, integral membrane proteins may differ from soluble proteins in the selection of suitable cross-linkers, which has never been investigated. In this study, we systematically evaluated the impact of five conventional cross-linkers targeting Lys, Asp and Glu, and two Arg-reactive cross-linkers on the structural and functional integrity of two G protein-coupled receptors (GPCRs). Perturbation of the receptor structure and ligand-binding activity was observed, depending on the receptor and crosslinking conditions. In particular, our study demonstrated that the concentrations of PDH and KArGO need to be fine-tuned in order to minimize the structural and functional disturbance of specific GPCRs. A set of amenable cross-linkers was selected to acquire the most comprehensive cross-link maps for two GPCRs. Our in-depth crosslinking mass spectrometry (CXMS) anal. has revealed dynamic features of structural regions in GPCRs that are not observable in the crystal structures. Thus, CXMS anal. of GPCRs using the expanded toolkit would facilitate structural modeling of uncharacterized receptors and gain new insights into receptor-ligand interactions.

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The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《The effect of carboxylic acid esters on the experimental hyperkinesis elicited by nicotine》. Authors are Liberman, S. S..The article about the compound:Sodium 4-butyl-3,5-dioxo-1,2-diphenylpyrazolidin-4-idecas:129-18-0,SMILESS:O=C(N(C1=CC=CC=C1)N2C3=CC=CC=C3)[C-](CCCC)C2=O.[Na+]).Product Details of 129-18-0. Through the article, more information about this compound (cas:129-18-0) is conveyed.

A study was made of the presence of a central nicotinolytic activity in the esters of diphenylacetic acid and its derivatives, which enhanced the resistance to nicotine and lowered the hyperkinesis produced by nicotine. Sixteen compounds were investigated. The dimethylaminoethyl ester of diphenylacetic acid proved the most active. In doses of 25 mg./kg. of body weight this compound prevented the death of the animals from nicotine and lowered the nicotinic hyperkinase to a considerable degree. The esters of benzilic acid, 2-quinuclidylmethyl, 4-pyridylmethyl, and isopropylaminoethyl esters of diphenylacetic acid proved ineffective in preventing nicotinic hyperkinesis. The results of the experiments led the author to conclude that the substitution of a H atom by a methyl group in a hydrocarbon radical which unites phenyl radicals has no substantial effect on the nicotinolytic activity of the compounds; the substitution of a hydroxyl group completely negated the nicotinolytic activity of the compounds

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Adrian, Rafael A.; Ibarra, Sara J.; Arman, Hadi D. published an article about the compound: Silver(I) trifluoromethanesulfonate( cas:2923-28-6,SMILESS:O=S(C(F)(F)F)([O-])=O.[Ag+] ).Recommanded Product: Silver(I) trifluoromethanesulfonate. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:2923-28-6) through the article.

The central AgI atom of the title salt, [Ag(INAM)2](CF3SO3)·2CH3CN, where INAM is isonicotinamide (C6H6N2O), is twofold coordinated by the pyridine N atoms of two isonicotinamide ligands creating a slightly distorted linear mol. geometry. The formation of polymeric chains {[Ag(INAM)2]+}n, held together by discrete hydrogen bonds through the amide group of the INAM ligand leaves voids for non-coordinating acetonitrile mols. that interact the silver metal center via regium bonds.

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Recommanded Product: 1260795-42-3. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: Methyl 4-bromo-2-formylbenzoate, is researched, Molecular C9H7BrO3, CAS is 1260795-42-3, about Discovery of Novel Inhibitors of LpxC Displaying Potent in Vitro Activity against Gram-Negative Bacteria. Author is Surivet, Jean-Philippe; Panchaud, Philippe; Specklin, Jean-Luc; Diethelm, Stefan; Blumstein, Anne-Catherine; Gauvin, Jean-Christophe; Jacob, Loic; Masse, Florence; Mathieu, Gaelle; Mirre, Azely; Schmitt, Christine; Lange, Roland; Tidten-Luksch, Naomi; Gnerre, Carmela; Seeland, Swen; Herrmann, Charlyse; Seiler, Peter; Enderlin-Paput, Michel; Mac Sweeney, Aengus; Wicki, Micha; Hubschwerlen, Christian; Ritz, Daniel; Rueedi, Georg.

UDP-3-O-((R)-3-hydroxymyristoyl)-N-glucosamine deacetylase (LpxC) is as an attractive target for the discovery and development of novel antibacterial drugs to address the critical medical need created by multidrug resistant Gram-neg. bacteria. By using a scaffold hopping approach on a known family of methylsulfone hydroxamate LpxC inhibitors, several hit series eliciting potent antibacterial activities against Enterobacteriaceae and Pseudomonas aeruginosa were identified. Subsequent hit-to-lead optimization, using cocrystal structures of inhibitors bound to Pseudomonas aeruginosa LpxC as guides, resulted in the discovery of multiple chem. series based on (i) isoindolin-1-ones, (ii) 4,5-dihydro-6H-thieno[2,3-c]pyrrol-6-ones, and (iii) 1,2-dihydro-3H-pyrrolo[1,2-c]imidazole-3-ones. Synthetic methods, antibacterial activities and relative binding affinities, as well as physicochem. properties that allowed compound prioritization are presented. Finally, in vivo properties of lead mols. which belong to the most promising pyrrolo-imidazolone series, such as I, are discussed.

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Benzofuran – Wikipedia,
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Ni, Yan; Li, Chun-Xiu; Wang, Li-Juan; Zhang, Jie; Xu, Jian-He published an article about the compound: (R)-Ethyl 4-chloro-3-hydroxybutanoate( cas:90866-33-4,SMILESS:O=C(OCC)C[C@@H](O)CCl ).Reference of (R)-Ethyl 4-chloro-3-hydroxybutanoate. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:90866-33-4) through the article.

A carbonyl reductase gene (yueD) from Bacillus sp. ECU0013 was heterologously overexpressed in Escherichia coli, and the encoded protein (BYueD) was purified to homogeneity and characterized. The NADPH-dependent reductase showed a broad substrate spectrum towards different aromatic ketones, and α- and β-ketoesters. Although the enantioselectivity was high to moderate for the reduction of α-ketoesters, all the tested β-ketoesters and aromatic ketones were reduced to the corresponding chiral alcs. in enantiomerically pure forms. Furthermore, the practical applicability of this enzyme was evaluated for the reduction of Et 4-chloro-3-oxobutanoate (1a). Using Escherichia coli cells coexpressing BYueD and glucose dehydrogenase, 215 g L-1 (1.3 M) of 1a was stoichiometrically converted to Et (R)-4-chloro-3-hydroxybutanoate ((R)-1b) in an aqueous-toluene biphasic system by using a substrate fed-batch strategy, resulting in an overall hydroxyl product yield of 91.7% with enantiomeric purity of 99.6% ee.

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Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

COA of Formula: C18H20N2O12. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, is researched, Molecular C18H20N2O12, CAS is 70539-42-3, about Covalent affinity labeling, detergent solubilization, and fluid-phase characterization of the rabbit neutrophil formyl peptide chemotaxis receptor. Author is Marasco, Wayne A.; Becker, Kathleen M.; Feltner, Douglas E.; Brown, C. Susan; Ward, Peter A.; Nairn, Roderick.

The formyl peptide chemotaxis receptor of rabbit neutrophils and purified rabbit neutrophil plasma membranes was identified by several affinity labeling techniques: (1) covalent affinity crosslinking of N-formyl-Nle-Leu-Phe-Nle-125I-Tyr-Lys (125I-hexapeptide) to the membrane-bound receptor with either di-Me suberimidate or ethylene glycol bis(succinimidyl succinate) and (2) photoactivation of N-formyl-Nle-Leu-Phe-Nle-125I-Tyr-Lys-Nε-6-[(4-azido-2-nitrophenyl)amino]hexanoate (125I-PAL). These techniques specifically identify the receptor as a polypeptide that migrates as a broad band on SDS-polyacrylamide electrophoresis, with a mol. weight (Mr) 50,000-65,000. The receptor was solubilized in active form from rabbit neutrophil membranes by using the detergents 3-[(3-cholamidopropyl)dimethylammonio]-1-propanesulfonate (CHAPS) and digitonin, and from whole cells with CHAPS. Chemotaxis receptor activity was measured by the ability of the solubilized membrane material to bind 125I-hexapeptide or N-formyl-Met-Leu-[3H]Phe with gel filtration or rapid filtration through poly(ethylenimine) (PEI)-treated filters as assay systems. 125I-PAL was specifically crosslinked to the same mol. weight material in the CHAPS and digitonin solubilized extract, but no specific labeling of the receptor was seen when membranes were extracted with Nonidet P-40 and Triton X-100. Therefore, although a large number of detergents are able to solubilize the receptor, apparently some detergents release the receptor in an inactive form. The ligand binding characteristics of formyl-Met-Leu-[3H]Phe to the CHAPS-solubilized receptor shared properties with the membrane-bound formyl peptide receptor, both of which showed curvilinear, concave-upward Scatchard plots. Computer curve fitting with the program NONLIN and statistical analyses of the binding data indicated that for both the membrane-bound and solubilized receptors a 2-saturable sites model fitted the data significantly better than did a 1-saturable site model. The characteristics of the 2-saturable sites model for the soluble receptor were: a high-affinity site with a KD value of 1.25 nM and a low-affinity site with a KD value of 19.77 nM. A total of 35% of the 2 sites detected was of the higher affinity. A Hill coefficient of 0.61 was observed

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The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: (R)-Ethyl 4-chloro-3-hydroxybutanoate(SMILESS: O=C(OCC)C[C@@H](O)CCl,cas:90866-33-4) is researched.COA of Formula: C18H20N2O12. The article 《Stereochemical control of microbial reduction. 2. Reduction of β-keto esters by immobilized bakers’ yeast》 in relation to this compound, is published in Tetrahedron Letters. Let’s take a look at the latest research on this compound (cas:90866-33-4).

Ketones in β-keto esters are reduced asym. by immobilized bakers’ yeast. The configuration and the enantiomer excess of the products were dramatically changed by the entrapment of yeast cells in dense polyurethane matrices.

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Synthetic Route of C19H19N2NaO2. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: Sodium 4-butyl-3,5-dioxo-1,2-diphenylpyrazolidin-4-ide, is researched, Molecular C19H19N2NaO2, CAS is 129-18-0, about Effect of meseclazone and other non-steroidal antiinflammatory drugs on isolated tracheal chain tone. Author is Diamantis, William; Melton, John L.; Sofia, R. Duane; Ciofalo, Vincent B..

Concentration-dependent relaxation of the isolated guinea pig tracheal chain was produced by the following nonsteroidal antiinflammatory drugs: naproxen [22204-53-1] > ibuprofen [15687-27-1] > diflunisal [22494-42-4] > tolmetin [26171-23-3] ≃ fenoprofen [29679-58-1] ≃ indomethacin [53-86-1] > phenylbutazone Na [129-18-0] > meseclazone (I) [29053-27-8] > 5-chlorosalicylic acid [321-14-2] > aspirin [50-78-2]. All these drugs were less potent than isoproterenol-HCl. This relaxation may be related to inhibition of prostaglandin synthesis, but since the relative potencies of the drugs in the tracheal test did not necessarily correspond to those in inhibiting prostaglandin synthetase in other tissues, other factors may be involved.

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The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate( cas:70539-42-3 ) is researched.HPLC of Formula: 70539-42-3.Ma, Xiuguang; Yuan, Dong; Diepold, Katharina; Scarborough, Tom; Ma, Jun published the article 《The Drosophila morphogenetic protein Bicoid binds DNA cooperatively》 about this compound( cas:70539-42-3 ) in Development (Cambridge, United Kingdom). Keywords: Bicoid protein cooperative DNA binding. Let’s learn more about this compound (cas:70539-42-3).

The Drosophila morphogenetic protein Bicoid, encoded by the maternal gene bicoid, is required for the development of the anterior structures in the embryo. Bicoid, a transcriptional activator containing a homeodomain, is distributed in an anterior-to-posterior gradient in the embryo. In response to this gradient, the zygotic gene hunchback is expressed uniformly in the anterior half of the embryo in a nearly all-or-none manner. In this report we demonstrate that a recombinant Bicoid protein binds cooperatively to its sites within a hunchback enhancer element. A less than 4-fold increase in Bicoid concentration is sufficient to achieve an unbound/bound transition in DNA binding. Using various biochem. and genetic methods we further demonstrate that Bicoid mols. can interact with each other. Our results are consistent with previous studies performed in the embryo, and they suggest that one mechanism to achieve a sharp on/off switch of gene expression in response to a morphogenetic gradient is cooperative DNA binding facilitated by protein-protein interaction.

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Benzofuran – Wikipedia,
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