- insecticide compositions, insecticidal products containing them and methods of eradicating pests using them
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Styryltriazole compounds having activity as antiparasitic hormone antagonists. Provided are an insecticide composition comprising an isomer or a pharmaceutically acceptable salt thereof, an insecticide product comprising the same, and a method for combating pests using the same.
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Paragraph 0147; 0154-0155; 0183; 0185-0188
(2021/01/29)
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- Application of poly(vinylphenyltrimethylammonium tribromide) resin as an efficient polymeric brominating agent in the α-bromination and α-bromoacetalization of acetophenones
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The applications of a new supported tribromide reagent based on poly(vinylbenzyltrimethylammonium hydroxide) resin (Amberlite 717) were reported. This supported tribromide resin was used directly in α-bromination and α-bromoacetalization of acetophenones without any other catalyst under mild conditions. The effects of solvents and the amount of the supported tribromide resin on the reactions were investigated. Under the optimal conditions, most of α-bromo and α-bromoacetal of acetophenones were selectively obtained in excellent yields.
- Han, Bingbing,Zheng, Zubiao,Zheng, Dongcheng,Zhang, Lei,Cui, Peng,Shi, Jianjun,Li, Changjiang
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supporting information
p. 2512 - 2520
(2019/07/04)
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- HEPATITIS C VIRUS INHIBITORS
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The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts thereof; to compositions containing such compounds; and to the of such compounds as inhibitors of HCV replication.
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- ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS
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Compounds represented by formula I as described herein or pharmaceutically acceptable salts thereof, wherein A, B, B', X, Y, R1, R2, R2', R3, R3', R4, R4', R5, R5', m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.
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Page/Page column 95
(2011/10/13)
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- Heme oxygenase inhibition by 1-Aryl-2-(1H-imidazol-1-yl/1H-1,2,4-triazol-1- yl)ethanones and their derivatives
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Previous studies by our research group have been concerned with the design of selective inhibitors of heme oxygenases (HO-1 and HO-2). The majority of these were based on a four-carbon linkage of an azole, usually an imidazole, and an aromatic moiety. In the present study, we designed and synthesized a series of inhibition candidates containing a shorter linkage between these groups, specifically, a series of 1-aryl-2-(1H-imidazol-1-yl/1H-1,2,4-triazol-1-yl) ethanones and their derivatives. As regards HO-1 inhibition, the aromatic moieties yielding best results were found to be halogen-substituted residues such as 3-bromophenyl, 4-bromophenyl, and 3,4-dichlorophenyl, or hydrocarbon residues such as 2-naphthyl, 4-biphenyl, 4-benzylphenyl, and 4-(2-phenethyl)phenyl. Among the imidazole-ketones, five (36-39, and 44) were found to be very potent (IC5050 in favor of HO-1. In the case of the azole-dioxolanes, two of them (80 and 85), each possessing a 2-naphthyl moiety, were found to be particularly potent and selective HO-1 inhibitors. Three non-carbonyl analogues (87, 89, and 91) of 1-(4-chlorophenyl)-2-(1H-imidazol-1-yl)ethanone were found to be good inhibitors of HO-1. For the first time in our studies, two azole-based inhibitors (37 and 39) were found to exhibit a modest selectivity index in favor of HO-2. The present study has revealed additional candidates based on inhibition of heme oxygenases for potentially useful pharmacological and therapeutic applications.
- Roman, Gheorghe,Vlahakis, Jason Z.,Vukomanovic, Dragic,Nakatsu, Kanji,Szarek, Walter A.
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experimental part
p. 1541 - 1555
(2011/11/29)
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- Lipid-lowering (hetero)aromatic tetrahydro-1,4-oxazine derivatives with antioxidant and squalene synthase inhibitory activity
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A number of newly synthesized 2-[4-(hetero)aromatic]phenyl-2-hydroxy- tetrahydro-1,4-oxazine derivatives were found to inhibit lipid peroxidation (IC50 of the most potent was 20 μM) as well as rat squalene synthase (IC50 for most between 1-10 μM). Antidyslipidemic action was demonstrated in vivo: the most active compound decreased triglycerides, total cholesterol, and LDL-cholesterol of hyperlipidemic rats by 64, 67, and 82%, respectively, at 56 μmol/kg (ip). Most of the novel compounds are more active than the structurally related and reference biphenyl-morpholine, pointing to useful structural approaches for the design of antiatherosclerotic agents.
- Kourounakis, Angeliki P.,Charitos, Christos,Rekka, Eleni A.,Kourounakis, Panos N.
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supporting information; experimental part
p. 5861 - 5865
(2009/09/25)
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- NITROGENOUS HETEROCYCLIC DERIVATIVE AND ORGANIC ELECTROLUMINESCENT ELEMENT EMPLOYING THE SAME
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A specific derivative of heterocyclic compound having nitrogen atom and an organic electroluminescence device comprising the compound. An organic electroluminescence device comprising at least one of organic compound layers including a light emitting layer sandwiched between an anode and a cathode, wherein said at least one of the organic compound layers comprises the derivative of the heterocyclic compound having nitrogen atom as a sole component or as mixed component. The organic electroluminescence device achieves elevation of luminance and excellent efficiency of light emission, and also achieves long lifetime by an improvement of an electrode adhesion.
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Page/Page column 86
(2008/06/13)
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- Sodium channel modulators derived from 2-piperidylimidazoles
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The invention concerns novel sodium channel modulators derived from 2-piperidylimidazoles. The inventive compounds correspond to the general formula (I), wherein: R1 represents a hydrogen atom or an —X—Y—R4 radical wherein —X—Y repre
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- PHENACYL ESTERS - A NEW TYPE OF LUQUID-CRYSTALLINE COMPOUND
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The reaction of aliphatic, alicyclic, and aromatic acids with 4-substituted α-bromoacetophenones gave a series of new liquid-crystalline phenacyl esters.Their mesomorphous characteristics are discussed in relation to the structures of the acid and ketone parts of the molecule.
- Torgova, S. I.,Karamysheva, L. A.,Agafonova, I. F.
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p. 1162 - 1168
(2007/10/02)
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- Stereochemical Course of an Enzyme-Catalyzed Allene-Acetylene Isomerization
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An allene-acetylene isomerase (AAI) isolated from hog liver interconverts the N-acetylcysteamine thio ester of 3-decynoic acid (3-decynoyl-NAC) and (+)-2,3-decadienoyl-NAC.It is thus far the only enzyme that has been isolated that produces (or utilizes) an allenic compound and that is not inactivated by that same allene.Although physical and kinetic characteristics of the enzyme have previously been obtained, details of its mechanism of action remain unknown.The stereochemical course of the AAI-catalyzed propalgylic rearrangement has now been determined, by synthesis of 2,3-- and 2,3- decadienoyl-NAC and enzymatic conversion of these substrates to 3-1>decanoyl-NAC.Derivatization of the chirality labeled acetylenes, followed by 2H NMR analysis, has shown that protonation occurs on the si face at C-2 of the allene.X-ray crystallographic analysis of a derivative has revealed that (+)-2,3-decadienoic acid possesses the S configuration.The enzyme-mediated propargylic rearrangement is therefore a suprafacial process, apparently involving a single active-site base.
- Schwab, John M.,Lin, Daniel C. T.
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p. 6046 - 6052
(2007/10/02)
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- ABSOLUTE CONFIGURATION OF AN ALLENIC ENZYME INACTIVATOR
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X-Ray crystallographic analysis of the 4-(4'-bromophenyl)phenacyl ester of (+)-2,3-decadienoic acid has shown that the allenic inhibitor of β-hydroxy-decanoylthioester dehydrase has the S configuration.
- Schwab, John M.,Lin, Daniel C. T.,He, Cun-heng,Clardy, Jon
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p. 4909 - 4912
(2007/10/02)
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