- Self-assembly of bistriazole BDT based bolaamphiphiles into SmA phase and helical organogels
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Bistriazole benzo[1,2-b:4,3-b′]dithiophene (BDT) contained bolaamphiphiles have been synthesized via Sonogashira coupling and click reactions as key steps. For such compounds, the central bent bistriazole BDT core, the flexible methylene spacer led the rodlike core together with the terminal diol groups to twist to be U-shaped polar region. Micro-segregation of U-shaped polar region from the lipophilic chains generated a SmA phase. Furthermore, these compounds can act as super organogelators to gel different kinds of solvents with the lowest critical gelation concentration (CGC) of 0.2 mg/ml. Gel morphologies with scarcely reported nanostructures including nanofibers, nanobelts, nanodisks, nanotrumpets and nanotubes were firstly observed in bolaamphiphilic self-assembly system.
- Cheng, Xiaohong,Gao, Hongfei,Liu, Yuantao,Yan, Qi,Zhang, Deling
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- Methanesulfinylation of Benzyl Halides with Dimethyl Sulfoxide
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A phenyltrimethylammonium tribromide-mediated nucleophilic substitution/oxygen transformation reaction of benzyl halides with DMSO has been developed. In this transition-metal-free reaction, DMSO acts as not only a solvent but also a "S(O)Me" source, thus providing a convenient method for the efficient and direct synthesis of various benzyl methyl sulfoxides.
- Fu, Duo,Dong, Jun,Du, Hongguang,Xu, Jiaxi
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p. 2752 - 2758
(2020/01/31)
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- COMPOUNDS, SALTS THEREOF AND METHODS FOR TREATMENT OF DISEASES
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The present disclosure relates to compounds according to Formula (I), useful for treating diseases.
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- Structure–Activity Relationship Studies of Vitamin D3 Analogues Containing an Ether or Thioether Linker as Hedgehog Pathway Inhibitors
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The Hedgehog (Hh) signaling pathway is critical for embryonic patterning and postembryonic tissue regeneration. Constitutive pathway activation has also been linked to human malignancies such as basal cell carcinoma (BCC) and medulloblastoma; therefore, multiple small-molecule scaffolds that inhibit Hh signaling are in development. Previously, Grundmann's alcohol, also known as the “northern region” of vitamin D3 (VD3), has been identified as a moderate Hh pathway inhibitor. In this study, isomers of Grundmann's alcohol with different orientations of the C4 hydroxy group and C3α proton were investigated to determine the optimal configuration for this hexahydroindane scaffold with respect to Hh inhibition. A series of analogues containing Grundmann's alcohol linked to a substituted phenyl or benzyl ring through an ether or thioether linker were synthesized and evaluated for their anti-Hh activity. Of these, analogue 17 ((1R,3aR,4R,7aR)-1-[(R)-1,5-dimethylhexyl]-4-(4-aminophenoxy)-7a-methyloctahydro-1H-indene) demonstrated potent anti-Hh activity in Hh-dependent BCC cells and did not activate canonical vitamin D receptor signaling, demonstrating its selective nature for the Hh signaling pathway.
- Wen, Jiachen,Hadden, M. Kyle
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supporting information
p. 748 - 753
(2018/03/05)
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- PERMEABLE GLYCOSIDASE INHIBITORS AND USES THEREOF
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Disclosed are compounds of Formula (I), wherein each substituent of Formula (I) is defined as in the specification, pharmaceutical formulations comprising these compounds which are useful as 0-linked N-acetylglucosaminidase (O-GlcNAcase) inhibitors, and thus are useful for the treatment of certain disorders such as Alzheimer' s disease including reducing NFTs and/or hyperphosphorylated tau. Also disclosed is the use of the compounds as O-GlcNAcase imaging agents.
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Page/Page column 77
(2013/12/03)
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- PERMEABLE GLYCOSIDASE INHIBITORS AND USES THEREOF
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The present invention is directed to compounds and pharmaceutical formulations comprising these compounds which are useful as O-linked N-acetylglucosaminidase (O-GlcNAcase) inhibitors, and thus may be useful for the treatment of certain disorders such as Alzheimer's disease including reducing NFTs and/or hyperphosphorylated tau. The invention is also directed to use of the compounds as O-GlcNAcase imaging agents.
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Page/Page column 77
(2013/12/03)
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- Fluorinated isatin derivatives. Part 2. New N-substituted 5-pyrrolidinylsulfonyl isatins as potential tools for molecular imaging of caspases in apoptosis
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Caspases are responsible for the execution of the cell death program and are potentially suitable targets for the specific imaging of apoptosis in vivo. A series of N-1-substituted analogues of the small molecule nonpeptide caspase inhibitor (S)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin (1), which may be useful for the development of caspase-targeted radioligands, were synthesized and their inhibition potencies were evaluated in vitro. Two of the most powerful techniques to introduce fluorine into organic compounds, viz, bromofluorination of olefins and fluorohydrin synthesis by ring-opening of epoxides, were used. Most of the target compounds are potent inhibitors of the two effector caspases-3 and -7. Furthermore, the 18F-radiolabeled model compound (S)-1-[4-(1-[18F]fluoro-2-hydroxyethyl)benzyl]-5-[1- (2-methoxymethyl-pyrrolidinyl) sulfonyl]isatin ([18F]37), a putative tracer for the noninvasive imaging of apoptosis by positron emission tomography (PET) was synthesized by nucleophilic epoxide ring-opening of its precursor 36. The radiochemistry utilized in the 18F-fluorination reverted to carrier-added [18F]Et3N·3HF, a new fluorine-18 source for radiolabeling.
- Podichetty, Anil K.,Wagner, Stefan,Schr?er, Sandra,Faust, Andreas,Sch?fers, Michael,Schober, Otmar,Kopka, Klaus,Haufe, Günter
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supporting information; experimental part
p. 3484 - 3495
(2010/03/03)
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- CARBOXAMIDE DERIVATIVES AS MUSCARINIC RECEPTOR ANTAGONISTS
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The invention relates to compounds of Formula (I) processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical composition containing them.
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Page/Page column 73
(2008/06/13)
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- Phenylpyridine derivatives
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The present invention relates to the compounds of formula I: their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical compositions containing such compoun
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Page/Page column 16
(2010/11/25)
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- Indole derivatives
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The present invention relates to the compounds of formula I: their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, compositions containing such compounds and their m
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Page/Page column 14-15
(2010/10/20)
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- Synthesis of model compounds for the investigation of biomarker's thermal behaviour
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The model compounds, which are used to investigate the organic structure and thermal behaviour of fossil fuels, have been synthesized starting from 4-hydroxybenzyl thiocholesterol, 4-hydroxybenzyl cholesterol and 4-hydroxybenzyl cholestanol.
- Sirkecioglu, Okan,Karliga, Bekir,Talinli, Naciye,Snape, Colin
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p. 1894 - 1899
(2007/10/03)
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- Novel pentafluorosulfanyl compounds
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The present invention provides the compounds of formula I-A their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical compositions containing th
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Page/Page column 17
(2010/02/13)
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- Novel oxidized thioether derivatives
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The present invention provides the compounds of formula I their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical compositions containing them
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Page/Page column 15
(2010/02/13)
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- Novel ether derivatives
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The present invention provides the compounds of formula (I) their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, compositions containing them and their man
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Page/Page column 9
(2010/02/14)
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- Eine orthogonale Glycosylierungsstrategie fuer den raschen Aufbau von Oligosacchariden an einem polymeren Traeger
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Keywords: Festphasensynthese; Glycoproteine; Glycosylierungen; Oligosaccharide
- Ito, Yukishige,Kanie, Osamu,Ogawa, Tomoya
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p. 2691 - 2693
(2007/10/03)
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- Rhodium(I)-centered cyclotriveratrylene
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The rigid bowl-shaped molecule cyclotriveratrylene (CTV,1) was provided with short and long spacer arms terminating in triphenyl phosphite functions.These CTV ligands were used to immobilize a rhodium(I)-carbonyl-hydride complex.The ligand with short spacers gave a rigid, strained complex with a trigonal-coordination sphere around the rhodium.The ligand with long flexible spacers allowed the formation of a large cavity after the complexation to the rhodium center.This cavity, however, is filled up by the spacer arms, as was indicated by NMR studies.Variable-temperature NMR experiments suggested that the H-Rh-CO dipole in the rhodium-CTV complex can adopt two orientations: one with the hydride group pointing away from the CTV cavity (low-temperature conformation) and one in which this orientation is inverted (high-temperature conformation).
- Coolen, H. K. A. C.,Reek, J. N. H.,Ernsting, J. M.,Leeuwen, P. W. N. M. van,Nolte, R. J. M.
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p. 381 - 386
(2007/10/03)
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