- Highly efficient and stable catalyst for peroxynitrite decomposition
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The new cobalt substituted-polyoxometalate K7[CoAlW11O39]·15H2O and the simple CoCl2·6H2O salt are efficient catalysts for peroxynitrite decomposition. These compounds also catalyze the oxidation of ascorbic acid and the nitration of phenol by peroxynitrite.
- Geletii,Bailey,Cowan,Weinstock,Hill
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Read Online
- Oxidation and reduction of nitrite ion in the TiO2 photo-induced catalytic reaction.
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During a photo-induced catalytic reaction under near UV irradiation to an aqueous suspension of Ti4O2, about 95% of NO2- was oxidized to NO3-, but NH4+ was not detected. The oxidation was inhibited by the addition of mannitol or under anaerobic conditions. The nitration of HPA was observed in the presence of t-buthanol, suggesting the formation of ONOO. An ESR spectrum gave a triplet signal at g = 2.041,in the presence of NO2-, mannitol, FeSO4, and MGD, indicating the reduction of NO2- to NO.
- Shibata,Noda,Ogura,Sogabe,Sawa
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- Catalase Catalyzes of Peroxynitrite-mediated Phenolic Nitration
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Catalase catalyzed the peroxynitrite-mediated nitration of 4-hydroxyphenylacetic acid. The curve for the pH dependence of nitration was similar to that for the reaction between peroxynitrite and phenol. Cyanide, azide, and 3-amino-1,2,4-triazole inhibited the nitration in a dose-dependent way. When catalase was mixed with peroxynitrite, Compound I was detected as an intermediate. Because azide was an electron donor for the peroxidatic action of catalase, and because 3-amino-1,2,4-triazole inhibited catalase activity by binding with Compound I, peroxynitrite-mediated phenolic nitration was probably accompanied by Compound I formation. Both catalase and superoxide dismutase protected Escherichia coli from peroxynitrite toxicity.
- Kono, Yasuhisa,Yamasaki, Tomoaki,Ueda, Akane,Shibata, Hitoshi
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Read Online
- COMPOUNDS, COMPOSITIONS AND METHODS FOR TREATING NASH, NAFLD, AND OBESITY
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The present technology relates to methods of treating NASH, NAFLD and/or obesity using compounds of Formulas I, II, III, IV, V, and/or VI. The methods include administering to a subject suffering from one or more of non-alcoholic steatohepatitis (NASH), non- alcoholic fatty liver disease (NAFLD) and/or obesity a therapeutically effective amount of such a compound
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Paragraph 00290
(2021/04/10)
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- PYRAZOLE-OXAZOLIDINONE COMPOUND FOR ANTI-HEPATITIS B VIRUS
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The present invention discloses a pyrazole-oxazolidinone compound having anti-hepatitis B virus activity, which has the structure of formula (I), wherein each variable is as defined herein.
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Paragraph 0290-0293
(2019/06/07)
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- Targeted probes of cellular physiology
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Biosensor comprising an activatable acceptor fluorogen linked via a linker to a donor which transfers energy to the fluorogen on detecting an analyte wherein the fluorogen component reacts and a 100 fold increase in intensity results when the fluorogen interacts non-covalently with an activator e.g. fluorogen activator peptide.
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Page/Page column 52
(2018/06/25)
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- NEW DIHYDRO-OXAZINOBENZODIAZEPINE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITONS CONTAINING THEM
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Compounds of formula (I) having a selective dual action on the central GABAergic system, and a process for their preparation and to pharmaceutical compositions containing them.
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Paragraph 0065
(2017/01/26)
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- NEW DIHYDRO-OXAZINOBENZODIAZEPINE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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Compounds of formula (I) wherein R1, R2 are independently selected from hydrogen and Cu alkyl; R3 is hydrogen or C1-4 alkyl group which is unsubstituted or substituted by phenyl, pyridyl, or amino optionally substituted by C1-4 alkyl; R4 is hydrogen; R5 is C1-4 alkyl group; R6 is selected from monocyclic aryl, which is a six membered ring unsubstituted or substituted by one or more identical or different groups selected from C1-4 alkyl groups, C1-4 alkoxy, halogenated C1-4 alkyl, phenyl, phenoxy, halogen, nitro; or mono- or bi- or tricyclic heteroaryl group consisting of five or six membered ring(s) having 1 to 3 identical or different hetero atoms selected from nitrogen, oxygen and sulfur, in which at least one of the rings is aromatic, and wherein the rings are optionally substituted by one or more identical or different groups selected from C1-4 alkyl, mono-, di-, tri- halogenated C1-4 alkyl, C1-4 alkoxy, hydroxyl, halogen; their positional isomers, racemates and enantiomers, diastereoisomers, and addition salts with a pharmaceutically acceptable acid, solvates, their complexes, adducts and prodrugs, having a selective dual action on the central GABAergic system, to a process for their preparation and to pharmaceutical compositions containing them.
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Page/Page column 16
(2015/08/06)
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- Reduction of the nitro group to amine by hydroiodic acid to synthesize o-aminophenol derivatives as putative degradative markers of neuromelanin
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Neuromelanin (NM) is produced in dopaminergic neurons of the substantia nigra (SN) and in noradrenergic neurons of the locus coeruleus (LC). The synthesis of NM in those neurons is a component of brain aging and there is the evidence that this pigment can be involved in the pathogenesis of neurodegenerative diseases such as Parkinson's disease. NM is believed to derive from the oxidative polymerization of dopamine (DA) or norepinephrine (NE) with the participation of cysteine, dolichols and proteins. However, there are still unknown aspects in the chemical structure of NM from SN (SN-NM) and LC (LC-NM). In this study, we designed a new method to synthesize o-aminophenol compounds as putative degradation products of catecholamines and their metabolites which may be incorporated into NM. Those compounds are aminohydroxyphenylethylamine (AHPEA) isomers, aminohydroxyphenylacetic acid (AHPAA) isomers and aminohydroxyethylbenzene (AHEB) isomers, which are expected to arise from DA or NE, 3,4-dihydroxyphenylacetic acid (DOPAC) or 3,4-dihydroxyphenylmandelic acid (DOMA) and 3,4-dihydroxyphenylethanol (DOPE) or 3,4- dihydroxyphenylethyleneglycol (DOPEG), respectively. These o-aminophenol compounds were synthesized by the nitration of phenol derivatives followed by reduction with hydroiodic acid (HI), and they could be identified by HPLC in HI hydrolysates of SN-NM and LC-NM. This degradative approach by HI hydrolysis allows the identification of catecholic precursors unique to SN-NM and LC-NM, which are present in catecholaminergic neurons.
- Wakamatsu, Kazumasa,Tanaka, Hitomi,Tabuchi, Keisuke,Ojika, Makoto,Zucca, Fabio A.,Zecca, Luigi,Ito, Shosuke
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p. 8039 - 8050
(2014/07/08)
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- COMPOUNDS AND METHODS
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The present invention relates to novel retinoid-related orphan receptor gamma (RORγ) modulators and their use in the treatment of diseases mediated by RORy.
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Page/Page column 103
(2013/03/26)
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- TARGETED PROBES OF CELLULAR PHYSIOLOGY
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Biosensor comprising an activatable acceptor fluorogen linked via a linker to a donor which transfers energy to the fluorogen on detecting an analyte wherein the fluorogen component reacts and a 100 fold increase in intensity results when the fluorogen interacts non-covalently with an activator e.g. fluorogen activator peptide.
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(2013/09/26)
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- SUBSTITUTED HETEROCYCLIC ACETAMIDES AS KAPPA OPIOID RECEPTOR (KOR) AGONISTS
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The present invention relates to a series of substituted compounds having the general formula (I), including their ste reoisomers and/or their pharmaceutically acceptable salts, wherein R1, R2, R3. R4, R5, and R6 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (κ) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.
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Page/Page column 90
(2013/09/26)
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- Compounds and Compositions for Modulating Lipid Levels and Methods of Preparing Same
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The present technology relates to compounds of Formulas I-VI and methods of making and using such compounds. Methods of use include prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, hepatic steatosis, and metabolic syndrome. Compounds disclosed herein also increase HDL-C, lower total cholesterol, LDL-cholesterol, and triglycerides and increase hepatic LDL receptor expression, inhibit PCSK9 expression, and activate AMP-activated protein kinase.
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Page/Page column 41-42
(2011/02/15)
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- CORYDALINE DERIVATIVES USEFUL FOR REDUCING LIPID LEVELS
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The present technology relates to compounds of Formulas (V) and (VI) and methods of making and using such compounds. Methods of use include prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, hepatic steatosis, and metabolic syndrome. Compounds disclosed herein also lower total cholesterol, LDL- cholesterol, and triglycerides and increase hepatic LDL receptor expression, inhibit PCSK9 expression, and activate AMP-activated potein kinase.
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Page/Page column 120
(2010/07/09)
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- Melanin-concentrating hormone antagonist
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A melanin-concentrating hormone antagonist comprising a compound of the formula: wherein R is hydrogen atom or a cyclic group which may be substituted; X is a bond or a spacer having a main chain of 1 to 10 atoms; Y is a spacer having a main chain of 1 to 6 atoms; ring A is benzene ring which may be further substituted; ring B is a 5- to 9-membered nitrogen-containing non-aromatic heterocyclic ring which may be further substituted; R1 and R2 are the same or different and are hydrogen atom, a hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; or R1 and R2, together with the adjacent nitrogen atom, may form a nitrogen-containing heterocyclic ring which may be substituted; or R2, together with the adjacent nitrogen atom and Y, may form a nitrogen-containing heterocyclic ring which may be substituted; or a salt thereof is useful as a preventive or therapeutic agent for obesity, etc.
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- Nitration and hydroxylation of substituted phenols by peroxynitrite. Kinetic feature and an alternative mechanistic view
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The reaction of peroxynitrite (ONOO-) with a series of para-substituted phenols has been examined in aqueous phosphate buffer and acetonitrile solutions. Major products were the corresponding 2-nitro derivative and the 4-substituted catechol. Kinetic study showed good correlation with Hammett σ(p)+ parameters and reduction potentials, suggesting the possible one-electron transfer process involving the nitrosoniun ion (NO+) as initial electrophile generated from peroxynitrous acid.
- Nonoyama, Nobuaki,Chiba, Kazuhiko,Hisatome, Kaori,Suzuki, Hitomi,Shintani, Futoshi
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p. 6933 - 6937
(2007/10/03)
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- Rigidized monomethine cyanines
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Boron complexes of certain bis-heterocyclic compounds are provided. The complexes resemble monomethine cyanines and are useful for imparting fluorescent properties to materials by covalent and noncovalent association. The compounds have the following general formula: STR1 wherein the dotted lines Z1 and Z2 represent the atoms necessary to complete a structure selected from the group consisting of one ring, two fused rings, and three fused rings, each said ring having five or six atoms, and each said ring comprising carbon atoms and, optionally, no more than two atoms selected from oxygen, nitrogen and sulfur, and R1 through R5 represent various atoms or groups and M is Cl or F.
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- β-lactams useful in determining the amount of elastase in a clinical sample
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Disclosed are β-lactams of formula I STR1 wherein X is a chromogenic or fluorogenic substituted aryl or heteroaryl, which are specific inhibitors of Human leukocyte elastase (HLE). Upon contact with HLE these compounds are cleaved to form a chromogenic or fluorogenic species which may be readily measured by the assay disclosed herein. The assay thus provides a means for direct measurement of the amount of active HLE in a body fluid or other sample.
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- Synthesis and Evaluation of Non-Catechol D-1 and D-2 Dopamine Receptor Agonists: Benzimidazol-2-one, Benzoxazol-2-one, and the Highly Potent Benzothiazol-2-one 7-Ethylamines
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Our interest in identifying D-1 and D-2 dopamine receptor agonists that are not catechols led us to extend previous studies with oxindoles by investigating analogues of dopamine, N,N-dipropyldopamine, m-tyramine, N,N-dipropyl-m-tyramine, and epinine in which the m-hydroxyl is replaced by the NH portion of a thiazol-2-one, oxazol-2-one, or imidazol-2-one group fused to the 2,3-position.These compounds were evaluated for their affinity and agonist activity at D-1 and D-2 receptors by using in vitro assays.Replacement of the m-hydroxy in N,N-dipropyldopamine with the thiazol-2-one group resulted in a dramatic increase in D-2 receptor affinity and activity compared to that of N,N-dipropyldopamine itself or that of the corresponding oxindole, 1.The resulting compound, 7-hydroxy-4-benzothiazol-2(3H)-one (4), is the most potent D-2 receptor agonist reported to date in the field-stimulated rabbit ear artery (ED50=0.028 nM).The benzoxazol-2-one (6), benzimidazol-2-one (5), and isatin (51) analogues showed D-2 receptor agonist potency similar to that of 1.The des-7-hydroxy analogues of 4 (21) also has enhanced D-2 receptor activity compared to that of the corresponding oxindole, 8. 7-Hydroxy-4-(2-aminoethyl)benzothiazol-2(3H)-one, 27, a non-catechol, has enhanced D-1 and D-2 receptor activity in vitro compared to that of the corresponding oxindole, 7.In vivo, 27 increased renal blood flow and decreased blood in the dog.However, these effects were mediated primarily by D-2 receptor agonist activity.This may be a result of the D-1 partial agonist activity of 27 coupled with its potent D-2 receptor activity.
- Weinstock, Joseph,Gaitanopoulos, Dimitri E.,Stringer, Orum D.,Franz, Robert G.,Hieble, J. Paul,et al.
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p. 1166 - 1176
(2007/10/02)
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- 4-[2-(dialkylamino)ethyl]-7-hydroxyisatins
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4-[2-(Dialkylamino)ethyl]-7-hydroxyisatins are prepared by internal condensation of an oxime followed by removal of protecting groups. The compounds are D2 -agonists and, thereby, have anti-hypertensive activity. A species of the group is 4-[2-(di-n-propylamino)ethyl]-4-hydroxyisatin.
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- A FACILE SYNTHESIS OF(+/-) 2-(4-CHLOROPHENYL)-α-METHYL-5-BENZOXAZOLACETIC ACID (BENOXAPROFEN)
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A convenient four step procedure for the synthesis of benoxaprofen is described starting with 4-hydroxyphenylacetic acid.
- Huegel, Helmut M.
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p. 1075 - 1080
(2007/10/02)
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- 7-(2-AMINOETHYL)-1,3-BENZTHIA- OR OXA-ZOL-2(3H)-ONES
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Certain aminoethyl substituted 1,3-benzthiazol-and 1,3-benzoxazol-2(3H)-ones are D 2-dopamine agonists. These compounds are prepared by reacting an appropriate o-aminophenol or thiophenol with phosgene.
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