272-12-8Relevant articles and documents
Thieno[2,3-c]pyridine, the first structure of a thienopyridine
Nerenz, Heiko,Grahn, Walter,Jones, Peter G.
, p. 787 - 789 (1997)
The title molecule, C7H5NS, is planar to within 0.009 A. Bond lengths at the heteroatoms are S1-C2 1.7276 (14), S1-C7a 1.7308 (13), N6-C5 1.354 and N6-C7 1.332 (2) A; the C-S-C angle is 90.76 (6)°. A libration analysis indicated corrections of 0.003-0.004 A. Short intermolecular contacts [S1...N6 3.229 (1) A] link the molecules into chains parallel to the y axis.
Synthesis and radioligand binding studies of C-5- and C-8-substituted 1-(3,4-dimethoxybenzyl)-2,2-dimethyl-1,2,3,4-tetrahydroisoquinoliniums as SK channel blockers related to N-methyl-laudanosine and N-methyl-noscapine
Graulich, Amaury,Scuvée-Moreau, Jacqueline,Seutin, Vincent,Liégeois, Jean-Fran?ois
, p. 4972 - 4982 (2007/10/03)
The synthesis and the 125I-apamin binding studies of original C-5- and C-8-substituted 1-(3,4-dimethoxy-benzyl)-2,2-dimethyl-1,2,3,4- tetrahydroisoquinoliniums and 1-(3,4-dimethoxy-benzyl)-6,6-dimethyl-4,5,6,7- tetrahydrothieno[2,3-c]pyridiniums were performed in order to find a reversible and selective SK channel blocker structurally related to N-methyl-laudanosine and N-methyl-noscapine. A bulky alkyl substituent in the C-8 position of the tetrahydroisoquinoline produces a clear increase in the affinity for the apamin sensitive binding sites. The presence of an electron-withdrawing group in the C-5 and C-8 positions is not a suitable substitution for the affinity of drugs structurally related to N-methyl-laudanosine. Thiophenic analogues and 8-methoxy derivatives possess a poor affinity for the apamin sensitive binding sites. Electrophysiological studies performed with the most effective compound showed a blockade of the apamin sensitive afterhyperpolarization in rat dopaminergic neurons.
FUNGAL CELL WALL SYNTHESIS GENE
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, (2008/06/13)
A reporter system reflecting the transport process that transports GPI-anchored proteins to the cell wall was constructed and compounds inhibiting this process were discovered. Further, genes conferring resistance to the above compounds were identified and methods of screening for compounds that inhibit the activity of the proteins encoded by these genes were developed.Therefore, through the novel compounds, the present invention showed that antifungal agents having a novel mechanism, i.e. inhibiting the process that transports GPI-anchored proteins to the cell wall, could be achieved.