17983-62-9Relevant academic research and scientific papers
Development of novel silicon-containing inverse agonists of retinoic acid receptor-related orphan receptors
Toyama, Hirozumi,Nakamura, Masaharu,Nakamura, Masahiko,Matsumoto, Yotaro,Nakagomi, Madoka,Hashimoto, Yuichi
, p. 1948 - 1959 (2014/03/21)
Retinoic acid receptor (RAR)-related orphan receptors (RORs) regulate a variety of physiological processes, including hepatic gluconeogenesis, lipid metabolism, circadian rhythm and immune function. The RAR agonist: all-trans retinoic acid was reported to be an RORβ inverse agonist, but no information is available regarding ROR activity of its synthetic analogue Am580. Therefore, we screened Am580 and some related tetramethyltetrahydronaphthalene derivatives and carried out structural development studies, including substitution of carbon atoms with silicon, with the aim of creating a potent ROR transcriptional inhibitor. The phenyl amide disila compound 22 showed the most potent ROR-inhibitory activity among the compounds examined. Its activity towards RORα, RORβ and RORγ was increased compared to that of Am580. The IC50 values for RORα, RORβ and RORγ are 1.3, >10 and 4.5 μM, respectively.
Application of a promiscuous Arthrobacter sp. from Antarctic in aerobic (R)-selective deracemization and anaerobic (S)-selective reduction
Palmeira, Dayvson J.,Arajo, Lidiane S.,Abreu, Juliana C.,Andrade, Leandro H.
, p. 117 - 125 (2015/02/19)
Inspired by enzyme-catalyzed reactions with microorganisms found in harsh marine environments, in which the amount of oxygen is restrict, we have shown that Arthrobacter sp. can perform different chemical transformations by switching from anaerobic to aerobic reaction conditions. Depending on the presence or absence of oxygen, either alcohol deracemization or ketone reduction with enantiocomplementary selectivities can be performed by the same microorganism. For example, reactions performed in the presence of oxygen favored the deracemization process, in which a racemic mixture of 1-(4-methylphenyl)ethanol was enriched to the (R)-alcohol in high conversion (94%) and high enantiomeric excess (94%). On the other hand, reaction in the absence of oxygen favored the reduction process, in which 4-methyl-acetophenone was converted to the (S)-alcohol in good conversion (58%) and excellent enantiomeric excess (>99%). These concepts were applied for both deracemization and enantioselective reduction of heteroatom-containing (silicon, phosphorus, tin and boron) molecules. Moreover, preparative scale reactions were also performed for both chemical processes.
Heterocyclic dihydrazole compounds and their use for controlling fungal plant diseases
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, (2008/06/13)
PCT No. PCT/US96/06533 Sec. 371 Date Nov. 13, 1997 Sec. 102(e) Date Nov. 13, 1997 PCT Filed May 8, 1996 PCT Pub. No. WO96/36633 PCT Pub. Date Nov. 21, 1996Compounds of Formula I, and their N-oxides and agriculturally suitable salts, are disclosed which ar
Enantioselective syntheses of 2-arylpropanoic acid non-steroidal antiinflammatory drugs and related compounds
Hamon, David P.G.,Massy-Westropp, Ralph A.,Newton, Josephine L.
, p. 12645 - 12660 (2007/10/02)
(S)-2-[4′-(2″-Methylpropyl)phenylpropanoic acid (ibuprofen) and (S)-2-(3′-benzoylphenyl)propanoic acid (ketoprofen) have been synthesised in high enantiomeric excess. Control of stereochemistry was achieved by a combination of Sharpless epoxidalion followed by catalytic hydrogenolysis of the introduced benzylic epoxide oxygen bond. Also, the coupling of organic compounds in the presence of palladium with enantiopure 2-(3-iodophenyl)propanoic and 2-(4-iodophenyl)propanoic acids, prepared by the methodology above, is a general method for the synthesis of optically active arylpropanoic acids.
Synthese d'aryl- et heteroarylsilanes par scission de l'hexamethyldisilane
Babin, P.,Bennetau, B.,Theurig, M.,Dunogues, J.
, p. 135 - 138 (2007/10/02)
In the presence of hexamethylphosphormaide and a catalytic quantity of tetrakis(triphenylphosphine)palladium, hexamethyldisilane reacts with various functional aryl bromides to give the corresponding arylsilanes in satisfactory yields.The reaction has bee
Retinobenzoic Acids. 5. Retinoidal Activities of Compounds Having a Trimethylsilyl or Trimethylgermyl Group(s) in Human Promyelocytic Leukemia Cells HL-60
Yamakawa, Takeru,Kagechika, Hiroyuki,Kawachi, Emiko,Hashimoto, Yuichi,Shudo, Koichi
, p. 1430 - 1437 (2007/10/02)
The retinoidal activities of trimethylsilyl or trimethylgermyl-containing retinobenzoic acids are discussed on the basis of differentiation-inducing activity on human promyelocytic leukemia cells HL-60.Compounds with a trimethylsilyl or trimethylgermyl gr
