- Synthesis of 9,9′-Spirobifluorenes and 4,5-Diaza-9,9′-spirobifluorenes and Their Application as Affinity Materials for Quartz Crystal Microbalances
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Two different classes of aza analogues of 9,9′-spirobifluorenes have been synthesized. These were obtained by either furnishing the spirobifluorene with additional pyridyl moieties or by installing the aza function directly into the spirobifluorene core. These structurally rigid compounds were then evaluated as affinity materials for quartz crystal microbalances and proved to be highly potent for the detection of volatile organic compounds.
- Stobe, Caroline,Pyka, Isabella,Linke, Alexander,Müller, Sarah,Schnakenburg, Gregor,Waldvogel, Siegfried R.,Lützen, Arne
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- Iridium(iii) complex-based electrochemiluminescent probe for H2S
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Since abnormal levels of hydrogen sulphide (H2S) correlate with various diseases, simple methods for its rapid and sensitive detection are highly required. Herein, we introduce a new electrochemiluminescent probe 1 for H2S based on a cyclometalated iridium(iii) complex. o-(Azidomethyl)benzoate ester groups on the main ligands of probe 1 react selectively with H2S, resulting in cascade reactions involving H2S-mediated reduction and intramolecular cyclization/ester cleavage. With this structural change induced by H2S, the intrinsic electrochemiluminescence (ECL) of 1 decreased greatly due to the unfavourable electron transfer of a tripropylamine (TPA) radical. Probe 1 showed a high ECL turn-off ratio and good selectivity for H2S over various anions and biothiols. The sensing mechanism of H2S was elucidated using1H NMR spectroscopy and MALDI-TOF mass spectrometry analyses.
- Park, Joonho,Kim, Taemin,Kim, Hoon Jun,Hong, Jong-In
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- METHODS OF USE FOR PYRIMIDINES AS FERROPORTIN INHIBITORS
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The subject matter described herein is directed to ferroportin inhibitor compounds of Formula (I) and pharmaceutical salts thereof, methods of preparing the compounds, pharmaceutical compositions comprising the compounds, and methods of administering the compounds for prophylaxis and/or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders, particularly iron overload states, such as thalassemia, sickle cell disease and hemochromatosis, and also kidney injuries.
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Paragraph 952; 954-956
(2021/11/06)
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- TRICYCLIC COMPOUNDS AND THEIR USE
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Tricyclic compounds and their use are provided. More specifically, tricyclic compounds, pharmaceutical compositions containing them, methods for preparing them, and their use in therapy are also provided.
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Page/Page column 78
(2020/12/29)
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- Synthesis of pyridine-N-oxide-borane intramolecular complexes by palladium-catalyzed reaction of 2-bromopyridine-N-oxides with alkynyltriarylborates
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Pyridine-N-oxide-borane intramolecular complexes having an aza-stilbene π-framework were synthesized by the palladium-catalyzed reaction of 2-bromopyridine-N-oxides with alkynyltriarylborates.
- Ishida, Naoki,Ikemoto, Wataru,Narumi, Mizuna,Murakami, Masahiro
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supporting information; experimental part
p. 3008 - 3011
(2011/08/05)
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- PYRIDINE DERIVATIVES USEFUL AS GLUCOKINASE ACTIVATORS
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Novel heterocyclic compounds of the formula (I) in which R1, R2, R3, R4 and D have the meanings indicated in Claim 1, are activators of glucokinase and can be used for the prevention and/o treatment of Diabetes Typ 1 and 2, obesity, neuropathy and/or nephropathy.
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Page/Page column 67
(2009/05/30)
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- Ring nitrogen-substituted non-steroidal estrogens: Pyridine and pyrimidine analogs of the phenol in deoxyhexestrol experience resonance constraints on preferred ligand conformation
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Pyridine and pyrimidine analogs of the non-steroidal estrogen deoxyhexestrol were synthesized. Their low affinity for the estrogen receptor is ascribed, in part, to resonance enforcement of a conformation unfavorable for binding. To develop compounds selective for estrogen receptor beta (ERβ), we substituted hydroxypyridine and pyrimidine heteroaryl groups for the characteristic phenol ring of non-steroidal estrogens. The unexpectedly low affinity showed by some of these compounds is ascribed, in part, to a resonance-enforced conformational constraint that prevents their optimal accommodation in the ER ligand binding pocket.
- De Angelis, Meri,Katzenellenbogen, John A.
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p. 5835 - 5839
(2007/10/03)
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- Intramolecular alkylation of aromatic compounds, XXXIV: Synthesis of pyridinylmethyl indolines as potential precursors of ergolines
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The carbinoles 3 prepared from the N-protected indolaldehydes 2 and bromomethoxypyridine 1 can smoothly be hydrogenolized to the lutidinylindoles 4 which in turn give the corresponding indolines 5 by NaCNBH3-reduction. Treatment of 3a by acid the trihetarylmethane 9 and 5-methoxypyridine-2-carboxaldehyde 10 are generated. The acetylpyridine 7 is found as a by-product of 3c. As by-product of the reduction the borane adduct 8 is detected.
- Reimann,Erdle
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p. 907 - 912
(2007/10/03)
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- Pyridyl and pyridazinyl substituted thyronine compounds having selective thyromimetic activity
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This invention relates to chemical compounds which have selective thyromimetic activity. A compound of this invention is 3,5-dibromo-3''-[6-oxo-3(1H)-pyridazinylmethyl]-thyronine.
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- Synthesis of Thyroid Hormone Analogues. Part 1. Preparation of 3'-Heteroarylmethyl-3,5-di-iodo-L-thyronines via Phenol-Dinitrophenol Condensation and Relationships between Structure and Selective Thyromimetic Activity
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3'-Heteroarylmethyl analogues (1)-(8) of the natural thyroid hormone 3,3',5-tri-iodo-L-thyronine (T3) were synthesized as potential selective (cardiac-sparing) thyromimetics.The diphenyl ether moiety was constructed by condensation of 3-substituted 4-methoxyphenols with a 3,5-dinitro-L-tyrosine derivative.Synthesis of the key phenols (28)-(32) required the in situ preparation, at low temperatures, of the novel metallated species 2-lithio-5-methoxypyridine (14), 5-lithio-2-methoxypyrimidine (15), 5-lithio-2-methylpyridine (16), 5-bromo-4-lithio-2-methoxypyridine (18) , and 2,6-difluoro-3-lithiopyridine (19), followed by reaction with the benzaldehyde (20).Alternative routes to the pyridazone (36) and thiazolone (37) phenols were developed from the benzyl bromide (33).Structure-activity relationships indicate that selective thyromimetic activity is associated with 2-oxyheteroaren-5-ylmethyl 3'-substitution, as found in the pyridone (1), pyridazinone (2), hydroxypyridine (4) and thiazolone (8).The location of the oxy substituent in the heterocycle is critical for both hormonal activity and for binding to the T3 receptor.
- Leeson, Paul D.,Emmett, John C.
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p. 3085 - 3096
(2007/10/02)
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