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Novel Chiral Phosphoramidite Monomers from (R)- and (S)-1,3-Butanediol: Synthesis of Modified Oligonucleotides and Binding Affinity Studies

Two optically active phosphoramidite monomers for modified oligodeoxyribo-nucleotides were prepared. These monomers were then introduced into dodecanucleotides in the middle of the sequences. The modified dodecanucleotides were characterized by various analytical methods including MALDI-TOF mass spectrometry and Tm values were obtained to appraise the binding affinity, by measuring change in UV absorbance at 260 nm.

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Reference£º
Synthesis and Crystal Structure of a Chiral?C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur¨Cnitrogen¨Coxygen ligand derived from aminothiourea and sodium?D-camphor-¦Â-sulfonate

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Massadine, a novel geranylgeranyltransferase type I inhibitor from the marine sponge Stylissa aff. massa

(Matrix presented) Massadine, a highly oxygenated alkaloid, was isolated from the marine sponge Stylissa aff. massa as an inhibitor of geranylgeranyltransferase type I (GGTase I). The structure of massadine has been deduced from spectral data. Massidine inhibited GGTase I from Candida albicans with an IC50 value of 3.9 muM.

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Reference£º
Synthesis and Crystal Structure of a Chiral?C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur¨Cnitrogen¨Coxygen ligand derived from aminothiourea and sodium?D-camphor-¦Â-sulfonate

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Volatile composition of Baga red wine: Assessment of the identification of the would-be impact odourants

Wines produced from Baga native variety from the Portuguese Bairrada Appellation, harvest 2000, were submitted to a liquid-liquid continuous extraction with dichloromethane and analysis by gas chromatography-mass spectrometry (GC-MS). A total of 53 compounds were identified and quantified. This wine has 225 mg l-1 volatile compounds, which include aliphatic and aromatic alcohols (44%), acids (27%), esters (15%), lactones (6%), amides (5%), and phenols (1%). To achieve the identification of the major would-be impact odourants, the aroma index was calculated using the concentration of each volatile component and the corresponding odour threshold reported in the literature. This methodology proved suitable, as a preliminary step, for the determination of the would-be impact odourants of Baga wine. From the 53 compounds identified, nine were determined as the most powerful odourants: guaiacol, 3-methylbutanoic acid, 4-ethoxycarbonyl-gamma-butyrolactone, isobutyric acid, 2-phenylethanol, gamma-nonalactone, octanoic acid, ethyl octanoate and 4-(1-hydroxyethyl)-gamma-butyrolactone. These data suggest Baga wine as a fruity-type product with an aroma correlated to a restricted number of compounds.

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Reference£º
Synthesis and Crystal Structure of a Chiral?C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur¨Cnitrogen¨Coxygen ligand derived from aminothiourea and sodium?D-camphor-¦Â-sulfonate

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Reference of 4254-15-3, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.4254-15-3, Name is (S)-Propane-1,2-diol, molecular formula is C3H8O2. In a article£¬once mentioned of 4254-15-3

Enantioselective synthesis of decarestrictine J

An efficient total synthesis of decarestrictine J has been achieved using ring-closing metathesis and Yamaguchi esterification as key steps. The stereogenic centres were generated by means of iterative hydrolytic kinetic resolution (HKR) of racemic epoxides.

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Reference£º
Synthesis and Crystal Structure of a Chiral?C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur¨Cnitrogen¨Coxygen ligand derived from aminothiourea and sodium?D-camphor-¦Â-sulfonate

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COMBINATION THERAPY FOR TREATING CYCLOOXYGENASE-2 MEDIATED DISEASES OR CONDITIONS IN PATIENTS AT RISK OF THROMBOTIC CARDIOVASCULAR EVENTS

The invention is directed to a method for treating a cyclooxygenase-2 mediated disease or condition in a mammalian patient at risk of a thrombotic cardiovascular event, wherein the patient is on aspirin therapy to reduce the risk of the thrombotic cardiovascular event, comprising orally concomitantly or sequentially administering to the patient a cyclooxygenase-2 selective inhibitor in an amount effective to treat the cyclooxygenase-2 mediate disease or condition, and a nitric oxide donating compound in accordance with Formula (I) or a pharmaceutically acceptable salt thereof, wherein the nitric oxide donating compound is administered in an amount effective to reduce the gastrointestinal toxicity caused by the combination of the cyclooxygenase-2 selective inhibitor and aspirin. Pharmaceutical compositions are also encompassed.

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Reference£º
Synthesis and Crystal Structure of a Chiral?C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur¨Cnitrogen¨Coxygen ligand derived from aminothiourea and sodium?D-camphor-¦Â-sulfonate

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Immobilized Aspergillus niger epoxide hydrolases: Cost-effective biocatalysts for the prepation of enantiopure styrene oxide, propylene oxide and epichlorohydrin

This study aimed to prepare robust immobilized epoxide hydrolase (EH) preparations for asymmetric hydrolysis of racemic epoxides such as styrene oxide, propylene oxide and epichlorohydrin. For this purpose, Aspergillus niger EH was immobilized onto Lewatit VP OC 1600 support by adsorption, modified Florisil and Eupergit C supports by covalently. The suitability of the supports was examined for protein binding capacity and rate of racemic styrene oxide hydrolysis. The protein-activity recovery yields were 75-85%, 82-78% and 90-75%, respectively for EH immobilized onto Lewatit VP OC 1600, modified Florisil and Eupergit C supports. All A. niger EH preparations catalyzed preferentially hydrolysis of (R)-epoxides. Although enantiomeric excess values of all the tested epoxides were 99%, the highest enantiopure epoxide yields were obtained as 48% for (S)-styrene oxide by the immobilized EHs onto modified Florisil and Eupergit C. The highest diol yield was obtained as 78% for 3-chloro-1,2-propanediol, however, its enantiomeric excess value was 28.2%. Enantioselectivity of A. niger EH was improved with the preparation of mentioned immobilized forms. The highest enantioselectivity value was obtained as 95 toward styrene oxide by A. niger EH immobilized onto modified Florisil . The results of reusability studies show that the immobilized EH preparations offer feasible potentials for the preparation of enantiopure epoxides than that of free form.

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Reference£º
Synthesis and Crystal Structure of a Chiral?C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur¨Cnitrogen¨Coxygen ligand derived from aminothiourea and sodium?D-camphor-¦Â-sulfonate

Simple exploration of (2S,3S)-Butane-2,3-diol

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Application of 19132-06-0, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.19132-06-0, Name is (2S,3S)-Butane-2,3-diol, molecular formula is C4H10O2. In a Article£¬once mentioned of 19132-06-0

Inhibition of topoisomerase II by ICRF-193, the meso isomer of 2,3-bis(2,6-dioxopiperazin-4-yl)butane: Critical dependence on 2,3-butanediyl linker absolute configuration

The bis(2,6-dioxopiperazine)s are a structurally and mechanistically unique class of topoisomerase II inhibitors that do not bind DNA and that do not stabilize topoisomerase II-DNA strand passing intermediates (“cleavable complexes”). The most effective topoisomerase II inhibitor in the bis(2,6-dioxopiperazine) series is ICRF-193 (meso or S*, R* isomer), with a meso 2,3-butanediyl linker connecting the dioxopiperazine rings. The two enantiomeric diastereomers, (R,R) and (S,S), of ICRF-193 possessing the two optically active 2,3-butanediyl linkers have been prepared from their respective optically pure 2,4-diaminobutanes via 2,3-diaminobutane-N,N,N?,N?-tetraacetic acid, esterification, and imide formation. Both in vivo and in vitro assays for catalytic inhibition of topoisomerase II were employed to show that the (S,S)-and (R,R)-isomers are almost inactive as topoisomerase II inhibitors. The data indicate that the meso stereochemistry of the alkanediyl linker is crucial for activity and provides additional evidence that the cytotoxicity of the bis(2,6-dioxopiperazine)s is due to their ability to inhibit topoisomerase II. Copyright

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Reference£º
Synthesis and Crystal Structure of a Chiral?C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur¨Cnitrogen¨Coxygen ligand derived from aminothiourea and sodium?D-camphor-¦Â-sulfonate

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Novel methods of manufacturing thromboxane A2 antagonists

This invention relates to several novel methods of manufacturing thromboxane A2 inhibiting 7-[3-alpha-[1-[[(phenylamino)-thioxomethyl]hydrazono]ethyl]-bicyclo[2.2.1]-heptenoic acids.

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Reference£º
Synthesis and Crystal Structure of a Chiral?C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur¨Cnitrogen¨Coxygen ligand derived from aminothiourea and sodium?D-camphor-¦Â-sulfonate

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Application of 4254-15-3, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 4254-15-3, molcular formula is C3H8O2, introducing its new discovery.

First asymmetric total synthesis of aspinolide A

The first total synthesis of aspinolide A has been achieved using ring-closing metathesis as a key step. The stereogenic centers were generated by means of hydrolytic kinetic resolution (HKR) of racemic epoxides.

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Reference£º
Synthesis and Crystal Structure of a Chiral?C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur¨Cnitrogen¨Coxygen ligand derived from aminothiourea and sodium?D-camphor-¦Â-sulfonate

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Preparation of Optically Active 1,2-Diols and alpha-Hydroxy Ketones Using Glycerol Dehydrogenase as Catalyst: Limits to Enzyme-Catalyzed Synthesis due to Noncompetitive and Mixed Inhibition by Product

Glycerol dehydrogenase (GDH, EC 1.1.1.6, from Enterobacter aerogenes or Cellulomonas sp.) catalyzes the interconversion of analogues of glycerol and dihydroxyacetone.Its substrate specificity is quite different from than of horse liver alcohol dehydrogenase (HLADH), yeast alcohol dehydrogenase, and other alcohol dehydrogenases used in enzyme-catalyzed organic synthesis and is thus a useful new enzymic catalyst for the synthesis of enantiomerically enriched and isotopically labeled organic molecules.This paper illustrates synthetic applications of GDH as a reduction catalyst by the enantioselective reduction of 1-hydroxy-2-propanone and 1-hydroxy-2-butanone to the corresponding R 1,2-diols (ee = 95-98percent). (R)-1,2-Butanediol-2-d1 was prepared by using formate-d1 as the ultimate reducing agent.Comparison of (R)-1,2-butanediol prepared by reduction of 1-hydroxy-2-butanone enzymatically and with actively fermenting bakers’ yeast indicated than yield and enantiomeric purity were similar by the two procedures.Reactions proceeding in the direction of substrate oxidation usually suffer from slow rates and incomplete conversions due to product inhibition.The kinetic consequences of product inhibition (competitive, noncompetitive, and mixed) for practical synthetic applications of GDH, HLADH, and other oxidoreductases are analyzed.In general, product inhibition seems the most serious limitation to the use of these enzymes as oxidation catalysts in organic synthesis.

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Reference£º
Synthesis and Crystal Structure of a Chiral?C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur¨Cnitrogen¨Coxygen ligand derived from aminothiourea and sodium?D-camphor-¦Â-sulfonate