- Fluxapyroxad Haptens and Antibodies for Highly Sensitive Immunoanalysis of Food Samples
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Fluxapyroxad is a new-generation carboxamide fungicide, with residues increasingly being found in food samples. Immunochemical assays have gained acceptance in food quality control as rapid, cost-effective, sensitive, and selective methods for large sample throughput and in situ applications. In the present study, immunoreagents to fluxapyroxad were obtained for the first time, and competitive immunoassays were developed for the sensitive and specific determination of fluxapyroxad residues in food samples. Two carboxyl-functionalized analogues of fluxapyroxad were prepared, and antibodies with IC50 values in the low nanomolar range were generated from both haptens, though a dissimilar response was observed concerning specificity. A robust direct assay was set up, with a calibration curve exhibiting a limit of detection of 0.05 nM (0.02 μg/L). Limits of quantitation of 5 μg/L were obtained for peach, apple, and grape juices using samples diluted in water. The direct immunoassay was also successfully applied to the determination of fluxapyroxad in grapes from in-field treated grapevines.
- Mercader, Josep V.,Abad-Somovilla, Antonio,Agulló, Consuelo,Abad-Fuentes, Antonio
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- Synthesis and 5-Lipoxygenase Inhibitory Activities of Eicosanoid Compounds
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Ten eicosanoid compounds (3, 6, 9, 11, 12, 15, 18, 21, 23, and 25), methyl (6E,8Z,11Z,14Z)-5-hydroxy-6,8,11,14-eicosatetraenoate (5-HETE, 10), leukotriene A4 (26), and (5S,6E,8E,10E,12RS,14E)-5,12-dihydroxy-6,8,10,14-eicosatetraenoic acid (5,12
- Arai, Yoshinobu,Shimoji, Katsuichi,Konno, Mitoshi,Konishi, Yoshitaka,Okuyama, Shigehiro,et al.
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- Of the trometamol prostaglandin F2 α synthesis method (by machine translation)
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The invention discloses a of the trometamol prostaglandin F2 α synthesis method, as the compound (-) - Corey lactone diol as raw materials, through the oxidation reaction to obtain lactone aldehyde, lactone aldehydechain after the weidiWeidi Greecehuo Naer reaction with - the lower side of the splicing an olefin, the olefin double-carbonyl after reduction to obtain the alcohol, with puncture ylide - wittich reaction the upper side of the obtained prostaglandin F2 α, then the prostaglandin F2 α of the trometamol after crystallization by dissolving of the trometamol prostaglandin F2 α. The synthesis method, without noble metal catalyst, there is little side reaction, high yield, low cost, less pollution, is suitable for industrial production. (by machine translation)
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Paragraph 0024
(2017/08/30)
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- Synthesis of a 10,000-membered library of molecules resembling carpanone and discovery of vesicular traffic inhibitors
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Split-and-pool synthesis of a 10,000-membered library of molecules resembling the natural product carpanone has been achieved. The synthesis features development of solid-phase multicomponent reactions between nitrogen nucleophiles, enones, and hydroxylamines, and a solid-phase application of the Huisgen cycloaddition affording substituted triazoles. The synthesis was performed in high-capacity (500 μm) polystyrene beads using a one bead-one stock solution strategy that enabled phenotypic screens of the resulting library. Using whole-cell fluorescence imaging, we discovered a series of molecules from the carpanone-based library that inhibit exocytosis from the Golgi apparatus. The most potent member of this series has an IC50 of 14 μM. We also report structure-activity relationships for the molecules exhibiting this interesting phenotype. These inhibitors of exocytosis may be useful reagents for the study of vesicular traffic.
- Goess, Brian C.,Hannoush, Rami N.,Chan, Lawrence K.,Kirchhausen, Tomas,Shair, Matthew D.
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p. 5391 - 5403
(2007/10/03)
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- BLOOD FLOW PROMOTERS FOR CAUDA EQUINA TISSUES
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It is intended to provide highly safe and efficacious blood flow promoters for cauda equina tissues. Among prostaglandin-like compounds having a weak hypotensive effect, compounds having an effect of promoting the blood flow in cauda equina tissues (excluding limaprost) are useful as highly safe blood flow promoters for cauda equina tissues and , therefore, are efficacious in preventing and/or treating lumbar pain, lower limb pain, lower limb palsy, intermittent claudication, vesicorectal failure, hypogonadism, etc. caused by cauda equina injuries.
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Page/Page column 28
(2010/11/23)
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- Macrocyclic polyamine lactones and derivatives thereof and their use as arthropod repellents
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The present invention describes an isolated macrocycle having the formula: where d is an integer from 0 to about 100; A, B, and each D are the same or different and are selected from the group consisting of each R1is the same or different and is a bivalent alkylene moiety; each R2is the same or different and is a bivalent alkylene moiety; and each R3is the same or different and is selected from the group consisting of a hydrogen atom and an alkyl moiety. Methods for producing these macrocycles are also described. The macrocycles of the present invention can be used as arthropod repellents.
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Page column 29
(2010/02/05)
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- Synthesis of [phenyl-2-3H]-travoprost: Isopropyl ester prodrug of a selective prostaglandin FP receptor agonist
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A method for the preparation of tritium labeled travoprost, a new ocular hypotensive prostaglandin, is described. A highly selective catalytic deiodination has been identified which provides [phenyl-2-3H]-travoprost in a single synthetic step f
- Selliah, Robert,Dantanarayana, Anura,Haggard, Karen,Egan, Judith,Do, Ernest U.,May, Jesse A.
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p. 173 - 183
(2007/10/03)
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- Novel Ring Cleavage Based on Intermolecular Aldol Condensation
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Ring cleavage and reconstruction via intramolecular aldol condensation followed by Grob fragmentation under acetalization conditions (BF3/ethylene glycol) was developed into a novel ring cleavage based on intermolecular aldol condensation.On the basis of
- Nagumo, Shinji,Matsukuma, Aki,Suemune, Hiroshi,Sakai, Kiyoshi
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p. 10501 - 10510
(2007/10/02)
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- Asymetric Diels-Alder Reactions with γ-Functionalized α,β-Unsaturated Chiral N-Acyloxazolidinones: Synthesis of (+)-S-145
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An extension of the asymmetric Diels-Alder cycloaddition with chiral γ-substituted, α,β-unsaturated imides is described.The application of these results to the synthesis of the potent TxA2 receptor antagonist (+)-S-145 was successfully achieved in a practical manner.
- Martinelli, Michael J.
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p. 5065 - 5073
(2007/10/02)
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- Quinolizidine Synthesis via Intramolecular Immonium Ion Based Diels-Alder Reactions: Total Syntheses of (+/-)-Lupinine, (+/-)-Epilupinine, (+/-)-Cryptopleurine, and (+/-)-Julandine
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Total syntheses of (+/-)-julandine (1), (+/-)-cryptopleurine (2), (+/-)-lupinine (3), and (+/-)-epilupinine (4) have been developed that feature intramolecular immonium ion based Diels-Alder reactions.Amines 6 and 14, prepared from stilbene ester 5 in a straightforward manner, gave rise to, upon treatment with aqueous formaldehyde solution, the corresponding immonium salts, which undergo intramolecular cyclocondensation, leading to isojulandine (11) and cryptopleurine (2), respectively, in good yield.Exposure of 11 to acid afforded (+/-)-julandine.Intramolecular cycloaddition of immonium ion 18 derived from amine 17 provided Diels-Alder adducts 19 and 20, which are rationalized on the basis of transition states 22 and 23, respectively.Reduction of 19 and 20 gave (+/-)-epilupinine (4) and (+/-)-lupinine (3), respectively.
- Grieco, Paul A.,Parker, David T.
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p. 3325 - 3330
(2007/10/02)
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- Synthesis of (15RS)-11-Deoxy-11-Oxacarbacyclin Methyl Ester
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(1R,2S,5S)-2-diphenyl-t-butylsiloxymethyl-3-oxabicyclooctan-7-one (3), prepared from D-ribonolactone, has been converted in six steps into the biologically active prostacyclin analogue (15RS)-11-deoxy-11-oxacarbacyclin methyl ester (2; X=O).
- Mann, John,Thomas, Alison
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p. 2287 - 2290
(2007/10/02)
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- Synthesis of the Prostaglandin H2 Analogue DL-9,11-Ethano-9,11-dideoxaprostaglandin H2
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The total synthesis of the prostaglandin H2 analogue, 9,11-ethano-9,11-dideoxaprostaglandin H2 (3), starting from the known Diels-Alder adduct (4) is described.
- Kametani, Tetsuji,Suzuki, Toshio,Kamada, Shinko,Unno, Katsuo
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p. 3101 - 3105
(2007/10/02)
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- Prostaglandin Analogues Possessing Antinidatory Effects. 2. Modification of the α Chain
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Additional double bonds were introduced into the α chain in 16-phenoxy-, 16-(3-chlorophenoxy)-, 16--, and 16-(4-chlorophenoxy)-17,18,19,20-tetranorprostaglandins which have antinidatory effects.Of these analogues, the Δ3/
- Hayashi, Masaki,Arai, Yoshinobu,Wakatsuka, Hirohisa,Kawamura, Masanori,Konishi, Yoshitaka,et al.
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p. 525 - 535
(2007/10/02)
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