- Triazolo and imidazo dihydropyrazolopyrimidine potassium channel antagonists
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Previously disclosed C6 amido and benzimidazole dihydropyrazolopyrimidines were potent and selective blockers of IKur current. Syntheses and SAR for C6 triazolo and imidazo dihydropyrazolopyrimidines series are described. Trifluoromethylcyclohexyl N(1) triazole, compound 51, was identified as a potent and selective Kv1.5 inhibitor with an acceptable PK and liability profile.
- Finlay, Heather J.,Jiang, Ji,Caringal, Yolanda,Kover, Alexander,Conder, Mary Lee,Xing, Dezhi,Levesque, Paul,Harper, Timothy,Hsueh, Mei Mann,Atwal, Karnail,Blanar, Michael,Wexler, Ruth,Lloyd, John
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supporting information
p. 1743 - 1747
(2013/04/10)
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- COMPOUNDS FOR FLUORESCENCE LABELING
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There are provided fluorescent compounds that can be used for DNA sequencing, measurement of physiologically active substance or the like based on fluorescence immunoassay and so forth. Compounds represented by the formula (I) (V1 to V5 represent a hydrogen atom or a functional group selected from the group consisting of a halogen atom, an alkyl group, an alkenyl group, a group that can form a covalent bond with a compound to be labeled and the like, and V1, V2 and others may bind to each other to form a saturated or unsaturated ring; R1 represents a hydrogen atom or a functional group selected from the group consisting of an alkyl group, an aryl group and a heterocyclic group; R3 and R4 represent an alkyl group, and R3 and R4 may bind to each other to form a ring; Q represents a group of atoms required to form a methine dye chromophore; and m and n represent 0 or 1, provided that m + n is 1) or salts thereof.
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- Novel (1H-1,2,3-triazol-1-yl)pyridines
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Pyridine ring substituted (1H-1,2,3-triazol-1-yl)pyridines were prepared and found to have insecticidal utility. 2-Chloro-6-(1H-1,2,3-triazol-1-yl)pyridine, for example, was prepared from 2-azio-6-chloropyridine and methyl propiolate by sequential condensation, hydrolysis, and decarboxylation and found to control aster leafhoppers.
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