- Synthesis and activities of a thienyl dihydropyridine series on intracellular calcium in a rat pituitary cell line (GH3/B6)
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The synthesis of a thienyl dihydropyridine series according to the Hantzsch method is described. The influence of these derivatives on intracellular calcium ([Ca2+](i)) in GH3 cells was evaluated in vitro using spectrofluorimetry with indol as Ca2+ fluorescent probe. We compared their effects on [Ca2+](i) and hormone release with those of nifedipine. The most active tested compounds on [Ca2+](i) were those methylated on the 3-position of the thienyl ring (activity was about 75% of nifedipine). Interestingly, the most efficient compounds on [Ca2+](i) were also the most efficient on hormone release.
- Varache-Lembege,Nuhrich,Zemb,Devaux,Vacher,Vacher,Dufy
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- The unexpected role of pyridine-2-carboxylic acid in manganese based oxidation catalysis with pyridin-2-yl based ligands
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A number of manganese-based catalysts employing ligands whose structures incorporate pyridyl groups have been reported previously to achieve both high turnover numbers and selectivity in the oxidation of alkenes and alcohols, using H2O2 as terminal oxidant. Here we report our recent finding that these ligands decompose in situ to pyridine-2-carboxylic acid and its derivatives, in the presence of a manganese source, H2O 2 and a base. Importantly, the decomposition occurs prior to the onset of catalysed oxidation of organic substrates. It is found that the pyridine-2-carboxylic acid formed, together with a manganese source, provides for the observed catalytic activity. The degradation of this series of pyridyl ligands to pyridine-2-carboxylic acid under reaction conditions is demonstrated by 1H NMR spectroscopy. In all cases the activity and selectivity of the manganese/pyridyl containing ligand systems are identical to that observed with the corresponding number of equivalents of pyridine-2-carboxylic acid; except that, when pyridine-2-carboxylic acid is used directly, a lag phase is not observed and the efficiency in terms of the number of equivalents of H 2O2 required decreases from 6-8 equiv. with the pyridin-2-yl based ligands to 1-1.5 equiv. with pyridine-2-carboxylic acid.
- Pijper, Dirk,Saisaha, Pattama,De Boer, Johannes W.,Hoen, Rob,Smit, Christian,Meetsma, Auke,Hage, Ronald,Van Summeren, Ruben P.,Alsters, Paul L.,Feringa, Ben L.,Browne, Wesley R.
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supporting information; experimental part
p. 10375 - 10381
(2011/01/09)
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- NOVEL ACTIVATORS OF GLUCOKINASE
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The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinsae activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistence and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.
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Page/Page column 143-145
(2009/04/25)
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- Thienyl substituted acylguanidines as inhibitors of bone resorption and vitronectin receptor antagonists
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Compounds of the formula and salts thereof wherein the substituents are defined as in accordance with the specification useful for the treatment of tumor growth, osteoporosis, inflammation and cardiovascular disorders.
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- Functionalized tetradentate ligands for Ru-sensitized solar cells
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Syntheses of 6,6′-bis(1-H-benzimidazol-2-yl)-4,4′-bis(methoxycarbonyl)- 2,2′-bipyridine and a series of new quaterpyridines as functionalized tetradentate ligands is described. A molecular engineering was developed allowing different solubilities, π-systems or grafting modes.
- Renouard, Thierry,Gr?tzel, Michael
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p. 8145 - 8150
(2007/10/03)
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- αvβ3 antagonists based on a central thiophene scaffold
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A series of novel, highly potent αvβ3 antagonists based on a thiophene scaffold and containing an acylguanidine as an Arg-mimetic is described. A number of structural features, such as cyclic versus open guanidine and a variety of li
- Peyman, Anusch,Scheunemann, Karl-Heinz,Will, David W.,Knolle, Jochen,Wehner, Volkmar,Breipohl, Gerhard,Stilz, Hans Ulrich,Carniato, Denis,Ruxer, Jean-Marie,Gourvest, Jean-Francois,Auberval, Marielle,Doucet, Bernard,Baron, Roland,Gaillard, Martine,Gadek, Thomas R.,Bodary, Sarah
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p. 2011 - 2015
(2007/10/03)
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- CHEMOSELECTIVE PROTECTION OF HETEROAROMATIC ALDEHYDES AS IMIDAZOLIDINE DERIVATIVES. PREPARATION OF 5-SUBSTITUTED FURAN- AND TIOPHENE-2-CARBOXALDEHYDES VIA METALLO-IMIDAZOLIDINE INTERMEDIATES
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Furan-, tiophene- and N-methylpyrrole-2-carboxaldehydes may be transformed into the corresponding N,N'-dimethylimidazolidines in a reaction not requiring acid catalysis.The resulting furan and tiophene (but not N-methylpyrrole) derivatives may be metallated in high yields and the carboxaldehyde functionality regenerated under very mild conditions.Treatment of the aldehydoketone 2-acetyl-5-formylthiophene with N,N'-dimethylethylenediamine gives only the product of reaction at the aldehyde function thus establishing this methodology as a potentially valuable method for the protection of an aldehyde in the presence of a ketone.
- Carpenter, Andrew J,,Chadwick, Derek J.
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p. 3803 - 3812
(2007/10/02)
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