Category: benzofurans

In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Synergism between acid and gastric contractile activity in the genesis of ulceration and hemorrhage in the phenylbutazone-treated rat, published in 1981-09-30, which mentions a compound: 129-18-0, mainly applied to phenylbutazone stomach ulcer mechanism, Name: Sodium 4-butyl-3,5-dioxo-1,2-diphenylpyrazolidin-4-ide.

The nonsteroid anti-inflammatory drugs including phenylbutazone produce significant gastric ulceration and hemorrhage even when administered by an extragastric route. To investigate the mechanism involved, cervical sectioned rats received an intraileal injection of phenylbutazone Na (I Na) [129-18-0] in methylcellulose. Gastric contractile activity was recorded with a miniature gastric balloon, and the stomach was perfused with either acid at pH 1 or buffer at pH 7. Rats receiving I developed a pattern of abnormally strong contractile activity that began 60-90 min after drug administration. The contracting stomachs of rats perfused with acid developed more ulceration and bled more severely than buffer-perfused rats. Vagotomy or atropine prevented the gastric contractile response to I, and such rats failed to develop significant ulceration in spite of the fact that their stomachs were perfused with acid. Cervical sectioned rats treated with methylcellulose alone failed to develop the abnormal contractile pattern and showed no significant gastric injury or hemorrhage. Thus, the focal hemorrhagic lesions induced by the extragastric administration of I in the rat are the result of mucosal compression at specific sites secondary to the passage of extremely strong peristaltic waves. They are vagally mediated and although the presence of acid does not appear essential for their initiation, it plays a synergistic role in their development and hemorrhage.

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In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Covalent labeling of vasopressin receptors from LLC-PK1 cells by the use of a bifunctional reagent, published in 1988-04-30, which mentions a compound: 70539-42-3, mainly applied to ethyleneglycolsuccinimidyl succinate vasopressin receptor complexation, Category: benzofurans.

The possibility of covalently attaching vasopressin to its receptors by the use of a bifunctional reagent was explored. Plasma membranes from the LLC-PK1 pig kidney cell line were purified by Percoll d. gradient centrifugation. These membranes contained a single population of high affinity (dissociation constant = 5.2 nM) and high maximum binding capacity (3.8 pmol/mg protein) [3H]lysine vasopressin ([3H]LVP)-binding sites. [3H]LVP-labeled receptors were solubilized with a high yield (83%) and minimal dissociation (9%) by treatment with the nonionic detergent, octaethylene glycol monododecyl ether (0.5%) in the presence of glycerol (20%). The solubilized [3H]LVP-labeled receptors were stable upon storage at 4° (5% dissociation after 24 h). They were partially purified to a specific activity of 17 pmol/mg of protein by chromatog. on a Cibacron blue-Sepharose column with a yield of 90%. The [3H]LVP-receptor complexes in both intact membranes and the partially purified preparation were almost completely dissociated by incubation at 30° for 30 min in the presence of 20 mM EDTA. This property was used to test the effect of ethylene glycol bis(succinimidyl-succinate) (EGS) as crosslinking reagent for the covalent attachment of [3H]LVP to its receptors. After treatment of [3H]LVP-labeled membranes for 30 min with 1 mM EGS at 4°, about 30% of specifically bound [3H]LVP was resistant to EDTA dissociation The amount of EDTA-resistant binding varied as a linear function of the fractional receptor occupancy and maximal binding capacity of the different batches of membranes used. Similar results were obtained with solubilized and partially purified vasopressin receptors. Upon steric exclusion HPLC, the EDTA-resistant [3H]LVP-labeled material, like the native [3H]LVP-labeled receptor, was eluted as a single and apparently homogeneous peak. The covalent character of the EGS-induced [3H]LVP binding to solubilized or partially purified receptors was assessed by its resistance to SDS-PAGE. The yield of EGS-induced labeling deduced from these experiments (27%) was close to that determined by the EDTA method. SDS-PAGE anal. of the [3H]LVP-labeled cross-linked material revealed the specific labeling of a major 50 kilodalton (kDa) component and a minor component of 30 kDa. The size of these 2 components was not affected by dithiothreitol.

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The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《Sequence of release of neurohormones on nervous stimulation of frog’s stomach muscle》. Authors are Singh, I..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+]).COA of Formula: C19H19N2NaO2. Through the article, more information about this compound (cas:129-18-0) is conveyed.

The experiments were performed on the stomach muscle of Rana tigrina. The nerve-muscle preparations were made as described by S., et al. (CA 56, 9285e), and were immersed in saline, or in 0.112M sucrose. The contraction produced by nerve stimulation showed seasonal variations. In summer (room temperature 29-31°), the latent period of response was 2-5 sec., and in winter (room temperature 23-5°), the latent period was 20-50 sec. In winter and in summer, atropine sulfate (I) did not abolish the contraction, unless it was previously treated with 2-bromo-D-lysergic acid diethylamide (II). Neopyramine (III) did not abolish the contraction of untreated muscles, but it abolished the contraction of muscles treated with I and II. The effects of II are different in summer and in winter. In winter, the contraction were diminished or abolished. In summer, the contractions were enhanced, but if the muscles were soaked in sucrose solution, the effect in summer was similar to that in winter. A combination of I, II, and III did not affect, or slightly diminished contractions in summer and in winter. If the muscle is soaked in sucrose, the contraction persists, indicating a release of substance P. Substance P itself caused contraction in sucrose-soaked muscles. As in winter, nervous stimulation in summer also produced relaxation, which was abolished by II the relaxation produced by adrenaline or noradrenaline was not affected.

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SDS of cas: 70539-42-3. 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 A high throughput dimer screening assay for monoclonal antibodies using chemical cross-linking and microchip electrophoresis. Author is Chen, Xiaoyu; Flynn, Gregory C..

A high throughput screening assay was developed to determine the total dimer level in antibody samples. This method utilizes high speed microchip electrophoresis separation following chem. crosslinking. Upon reacting with homobifunctional N-hydroxysuccinimide-esters (NHS-esters), covalent linkages can be established between the primary amines of two neighboring antibody mols. The reaction conditions are optimized to achieve quant. crosslinking of only phys. associated monomers within an antibody dimer. The resulting crosslinked dimers, originating from either covalent or non-covalent antibody dimers, can then be separated from monomers by SDS electrophoresis. A com. microchip electrophoresis instrument is used for high speed separation, allowing each sample to be analyzed in about 1 min. This approach was applied to crude mammalian cell culture samples. Using a 96-well gel filtration spin column format, interfering species in the cell culture media were efficiently removed from the samples. This method is well suited to the purpose of high throughput antibody dimer quantitation during cell culture expression, including clone selection and cell culture development. The total dimer content, both covalent and non-covalent, can be determined for hundreds of crude samples in a few hours. The effects of different crosslinking conditions on the determined dimer levels, as well as of different antibody pI values, are discussed.

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Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 129-18-0, is researched, SMILESS is O=C(N(C1=CC=CC=C1)N2C3=CC=CC=C3)[C-](CCCC)C2=O.[Na+], Molecular C19H19N2NaO2Journal, Bulletin of the Faculty of Pharmacy (Cairo University) called Formulation and stabilization of phenylbutazone sodium injectable solution, Author is Kassem, Aly Aly; Abd El-Bary, Ahmed, the main research direction is phenylbutazone sodium injection stabilization.Recommanded Product: Sodium 4-butyl-3,5-dioxo-1,2-diphenylpyrazolidin-4-ide.

The most appropriate pH for phenylbutazone sodium solutions is 8.2. Sterilization at 100° for 30 min in the presence of 0.2% chlorocresol is the most satisfactory. Light has a deleterious effect on this solution The stability of the product improves in the presence of propylene glycol,sodium metabisulfite and diethylenetriaminepentaacetic acid. The use of the antioxidant and the complexing agent in combination gave better results than the use of either of these alone.

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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.Recommanded Product: Ethyl 2-(2-oxopyrrolidin-1-yl)acetate. The article 《Efficient synthesis of optically pure alcohols by asymmetric hydrogen-transfer biocatalysis: application of engineered enzymes in a 2-propanol-water medium》 in relation to this compound, is published in Applied Microbiology and Biotechnology. Let’s take a look at the latest research on this compound (cas:90866-33-4).

An efficient method is described for producing both enantiomers of chiral alcs. by asym. hydrogen-transfer bioreduction of ketones in a 2-propanol (IPA)-water medium with Escherichia coli biocatalysts expressing phenylacetaldehyde reductase (PAR: wild-type and mutant enzymes) from Rhodococcus sp. ST-10 and alc. dehydrogenase from Leifsonia sp. S749 (LSADH). Also described are the detailed properties of mutant PARs, Sar268, and HAR1, which were engineered to have high activity and productivity in media composed of polar organic solvent and water, and the construction of three-dimensional structure of PAR by homol. modeling. The Km and Vmax values for some substrates and the substrate specificity of mutant PARs were quite different from those of wild-type PAR. The results well explained the increased productivity of engineered PARs in IPA-water medium.

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Recommanded Product: 2923-28-6. 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: Silver(I) trifluoromethanesulfonate, is researched, Molecular CAgF3O3S, CAS is 2923-28-6, about Stimuli-Responsive Topological Transformation of a Molecular Borromean Ring via Controlled Oxidation of Thioether Moieties. Author is Zhang, Hai-Ning; Yu, Wei-Bin; Lin, Yue-Jian; Jin, Guo-Xin.

A Cp*-Rh based D-shaped binuclear metallacycle and a template-free mol. Borromean ring (BR) were obtained in high yield using the semi-rigid thioether dipyridyl ligand 1,4-bis[(pyridin-4-ylthio)methyl]benzene (Bptmb). The topol. transformation from a binuclear metallacycle and a BR to tetranuclear metallacycles was realized via the controlled oxidation of thioethers. The strategy used in this work can be regarded as a new form of stimuli-responsive post-synthesis modification (PSM).

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The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《N-[5-(2-Methoxyethoxy)-2-pyrimidinyl] benzenesulfonamide (glycodiazine). V. Effect of phenylethylbarbituric acid on the metabolism and hypoglycemic effect of glycodiazine in vitro and vivo》. Authors are Gerhards, E.; Kolb, K. H.; Schulze, P. E..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+]).Name: Sodium 4-butyl-3,5-dioxo-1,2-diphenylpyrazolidin-4-ide. Through the article, more information about this compound (cas:129-18-0) is conveyed.

cf. CA 64, 18224g. The metabolism of glycodiazine, 2-benzenesulfonamido-5-(βhydroxyethoxy)diazine (II), and tolbutamide after Luminal treatment was studied in the rat, dog, and in man. The 20,000 g liver supernatant from untreated rats metabolized 25% of the glycodiazine and tolbutamide in vitro, whereas that fraction from rats treated with Luminal (2 × 5 mg./100 g. body weight/ day for 3 days intraperitoneally) metabolized 60-70% of the drugs. The formation of 2-benzenesulfonamido-5-(carboxymethoxy)diazine from II was increased from 2% with liver fractions from untreated rats to 8% with that from Luminal-treated rats. After oral administration of glycodiazine-3H to untreated rats, 35% of the radioactivity was excreted in the urine within the 1st 4 hrs., whereas Luminal-treated rats excreted 65%. Pretreatment of dogs with Luminal (10 mg./kg./ day for 7 days orally) increased the urinary excretion of 3H following oral administration of 900 mg. of glycodiazine-3H 1.6-fold within 12 hrs., compared with nonpretreated controls. Luminal did reduce the concentration of glycodiazine in the blood, however. In man, pretreatment with Luminal reduced the level of glycodiazine about 2-fold when compared with controls. Luminal did not affect the hypoglycemic effect of glycodiazine in rats, dogs, or humans, indicating that the former has no effect on the influence of the latter on insulin secretion. 23 references.

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Related Products of 129-18-0. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: Sodium 4-butyl-3,5-dioxo-1,2-diphenylpyrazolidin-4-ide, is researched, Molecular C19H19N2NaO2, CAS is 129-18-0, about Pharmacological properties of butazolidine and of its calcium and sodium salts. Author is Wilhelmi, G..

The antiinflammatory effect of butazolidine Ca (I) was compared with that of butazolidine (II) and of its Na salt (III). I had a less potent effect than II or III against formalin peritonitis in the rat and ultraviolet erythema in the guinea pig. It showed a potency equal to II and III against formalin edema in the rat and croton oil inflammation in the mouse ear. I was more effective than II or III with respect to inhibition of exudation in the granuloma pouch.

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Recommanded Product: 134434-31-4. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: Isoquinolin-3-ol, is researched, Molecular C9H7NO, CAS is 134434-31-4, about Direct-dynamics approach to catalytic effects: The tautomerization of 3-hydroxyisoquinoline as a test case. Author is Fernandez-Ramos, Antonio; Smedarchina, Zorka; Zgierski, Marek Z..

The mechanism of tautomerization of 3-hydroxyisoquinoline (3HIQ) in its first excited singlet state is studied theor. for the isolated mol. and the 1:1 complexes with water (3HIQ/H2O) and acetic acid (3HIQ/AA). It is found that the proton transfer is a tunneling process which is strongly mediated by the motion of the heavier atoms involved in the hydrogen bond bridges. Therefore it is argued that quant. assessment of the tremendous catalytic effect of complexation observed exptl. is possible only through the evaluation of multidimensional tunneling rate constants These are addressed using a direct dynamics approach based on the multidimensional instanton model. The potential energy surface, which governs the tautomerization dynamics, is generated from ab initio calculations at CIS/6-31G* and CASSCF(8,8)/6-31G* levels of theory. It is formulated in terms of the normal modes of the transition state and consists of 33, 57, and 72 degrees of freedom for 3HIQ, 3HIQ/H2O, and 3HIQ/AA, resp. The catalytic effect of complexation is discussed as an interplay between the static component, reflected in the change of geometries and relative stabilities of the three stationary points, and the dynamic one, resulting from the effects of coupling of the tunneling motion to the skeletal modes. Since the coupling parameters reported in the present study are typical for proton transfer along hydrogen bridges, the relative weight of these effects in the overall acceleration of the reaction will be larger in complexes with smaller reduction of the barrier height upon complexation.

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