- Oxidation of aromatic and aliphatic aldehydes to carboxylic acids by Geotrichum candidum aldehyde dehydrogenase
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Oxidation reaction is one of the most important and indispensable organic reactions, so that green and sustainable catalysts for oxidation are necessary to be developed. Herein, biocatalytic oxidation of aldehydes was investigated, resulted in the synthesis of both aromatic and aliphatic carboxylic acids using a Geotrichum candidum aldehyde dehydrogenase (GcALDH). Moreover, selective oxidation of dialdehydes to aldehydic acids by GcALDH was also successful.
- Hoshino, Tomoyasu,Yamabe, Emi,Hawari, Muhammad Arisyi,Tamura, Mayumi,Kanamaru, Shuji,Yoshida, Keisuke,Koesoema, Afifa Ayu,Matsuda, Tomoko
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- NOVEL COMPOUNDS
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Heterocyclic compounds and salts according to formula (I), which are pyrimidinone derivatives, described herein exhibit human neutrophil elastase inhibitory properties, and useful for treating diseases or conditions in which HNE is implicated.
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- TETRAHYDROTRIAZOLOPYRIMIDINE DERIVATIVES AS HUMAN NEUTROPHIL ELASTASE INHIBITORS
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This invention relates to heterocyclic compounds, which are pyrimidinone derivatives having human neutrophil elastase inhibitory properties, and their use in therapy.
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- NOVEL COMPOUNDS
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This invention relates to heterocyclic compounds, which are pyrimidinone derivatives having human neutrophil elastase inhibitory properties, and their use in therapy.
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- NOVEL COMPOUNDS
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Compounds of formula (I), described herein, exhibit human neutrophil elastase inhibitory properties, and are useful for the treatment of diseases and conditions in which HNE is implicated.
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- NOVEL COMPOUNDS
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Compounds of formula (I) defined herein exhibit human neutrophil elastase inhibitory properties and are useful for treating diseases and conditions in which HNE is implicated.
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- NOVEL COMPOUNDS
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This invention relates to heterocyclic compounds, which are pyrimidinone derivatives having human neutrophil elastase inhibitory properties, and their use in therapy.
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- Modeling, Synthesis and Biological Evaluation of Potential RetinoidX Receptor-Selective Agonists: Novel Halogenated Analogues of 4-[1-(3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic Acid (Bexarotene)
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The synthesis of halogenated analogues of 4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic acid (1), known commonly as bexarotene, and their evaluation for retinoidX receptor (RXR)-specific agonist performance is described. Compound 1 is FDA approved to treat cutaneous T-cell lymphoma (CTCL); however, bexarotene treatment can induce hypothyroidism and elevated triglyceride levels, presumably by disrupting RXR heterodimer pathways for other nuclear receptors. The novel halogenated analogues in this study were modeled and assessed for their ability to bind to RXR and stimulate RXR homodimerization in an RXRE-mediated transcriptional assay as well as an RXR mammalian-2-hybrid assay. In an array of eight novel compounds, four analogues were discovered to promote RXR-mediated transcription with EC50 values similar to that of 1 and are selective RXR agonists. Our approach also uncovered a periodic trend of increased binding and homodimerization of RXR when substituting a halogen atom for a proton ortho to the carboxylic acid on 1.
- Furmick, Julie K.,Kaneko, Ichiro,Walsh, Angela N.,Yang, Joanna,Bhogal, Jaskaran S.,Gray, Geoffrey M.,Baso, Juan C.,Browder, Drew O.,Prentice, Jessica L.S.,Montano, Luis A.,Huynh, Chanh C.,Marcus, Lisa M.,Tsosie, Dorian G.,Kwon, Jungeun S.,Quezada, Alexis,Reyes, Nicole M.,Lemming, Brittney,Saini, Puneet,vanderVaart, Arjan,Groy, Thomas L.,Marshall, Pamela A.,Jurutka, Peter W.,Wagner, Carl E.
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p. 1551 - 1566
(2012/11/07)
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- Solid-phase combinatorial synthesis of benzothiazoles, benzimidazoles, and benzoxazoles using a traceless linker
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New methodology for the solid-phase synthesis of benzothiazoles, benzimidazoles, and benzoxazoles has been developed by using a traceless 4-alkoxy-aniline linker. The desired products were released from the polymer support by imine-exchange process couple
- Hioki, Hideaki,Matsushita, Kimihito,Kubo, Miwa,Harada, Kenichi,Kodama, Mitsuaki,Fukuyama, Yoshiyasu
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p. 11315 - 11324
(2008/03/12)
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