- Discovery and SAR of 2-arylbenzotriazoles and 2-arylindazoles as potential treatments for Duchenne muscular dystrophy
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Families of 2-arylbenzotriazoles and 2-arylindazoles that show positive effects in screens predictive of endogenous utrophin upregulation have been identified. Synthesis and structure-activity relationships are described leading to compounds with attractive in vitro profiles.
- De Moor, Olivier,Dorgan, Colin R.,Johnson, Peter D.,Lambert, Adam G.,Lecci, Cristina,Maillol, Carole,Nugent, Gary,Poignant, Severine D.,Price, Paul D.,Pye, Richard J.,Storer, Richard,Tinsley, Jonathon M.,Vickers, Richard,Well, Renate Van,Wilkes, Fraser J.,Wilson, Francis X.,Wren, Stephen P.,Wynne, Graham M.
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p. 4828 - 4831
(2011/09/16)
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- TREATMENT OF DUCHENNE MUSCULAR DYSTROPHY
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There are disclosed compound of Formula (I) or (II) wherein A1, A2, A3, A4and A5, which may be the same or different, represent N or CR1, R9 represents - L -R3, in whi
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Page/Page column 30
(2010/11/28)
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- APPLICATION OF FLUORESCENT TRIAZOLES TO ANALYTICAL CHEMISTRY. III. FLUORESCENCE CHARACTERISTICS OF 2-PHENYLBENZOTRIAZOLYL-5-AMINE DERIVATIVES AS FLUORESCENT PROBES
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2-Phenylbenzotriazole derivatives with a COCH3 or NH2 group on the 2-phenyl ring were synthesized and found to be applicable as fluorescent hydrophobic probes.The fluorescence intensities of these compounds, which were intense in non-polar solvents, were dramatically quenched in polar solvents.In particular, 2-(4-acetylphenyl)-2H-benzotriazolyl-5-amine (7) showed a much higher ratio of the fluorescence intensity in the organic solvent to that in water (Fo/Fw) than 8-anilino-1-naphthalenesulfonate (ANS): The Fo/Fw values of 7 were 470 for dioxane and 440 for acetone, while those of ANS were 100 for dioxane and 90 for acetone.We modified compound 7 to obtain water-soluble probes for use in drug-protein binding studies and examined the interaction of these probes with human serum albumin (HSA).All the compounds, which were practically non-fluorescent in the buffer solution, bound to HSA and fluoresced.Keywords: 2-phenylbenzotriazolyl-5-amine; fluorescence characteristies; solvent effect; fluorescent probe; protein binding
- Narita, Shigeru,Kitagawa, Takayasu
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p. 1005 - 1008
(2007/10/02)
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