4345-23-7Relevant academic research and scientific papers
Discovery of 2-arylbenzoxazoles as upregulators of utrophin production for the treatment of duchenne muscular dystrophy
Chancellor, Daniel R.,Davies, Kay E.,De Moor, Olivier,Dorgan, Colin R.,Johnson, Peter D.,Lambert, Adam G.,Lawrence, Daniel,Lecci, Cristina,Maillol, Carole,Middleton, Penny J.,Nugent, Gary,Poignant, Séverine D.,Potter, Allyson C.,Price, Paul D.,Pye, Richard J.,Storer, Richard,Tinsley, Jonathon M.,Van Well, Renate,Vickers, Richard,Vile, Julia,Wilkes, Fraser J.,Wilson, Francis X.,Wren, Stephen P.,Wynne, Graham M.
supporting information; experimental part, p. 3241 - 3250 (2011/07/06)
Figure Presented. A series of novel 2-arylbenzoxazoles that upregulate the production of utrophin in murine H2K cells, as assessed using a luciferase reporter linked assay, have been identified. This compound class appears to hold considerable promise as a potential treatment for Duchenne muscular dystrophy. Following the delineation of structure-activity relationships in the series, a number of potent upregulators were identified, and preliminary ADME evaluation is described. These studies have resulted in the identification of 1, a compound that has been progressed to clinical trials.
TREATMENT OF DUCHENNE MUSCULAR DYSTROPHY
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Page/Page column 51; 58, (2008/06/13)
There are disclosed compound of Formula (1): A1, A2, A3 and A4 which may be the same or different, represent N or CR1, X is a divalent group selected from O, S(O)n, C=W, NR4, NC(=O)R5 and CR6R7, W is O, S, NR20, Y is N or CR8, one of R4, R5, R6, R8, R9 and NR20 represents - L -R3, in which L is a single bond or a linker group, additionally, R1, R3 - R9, which may be the same or different, independently represent hydrogen or a substituent and R20 represents hydrogen, hydroxyl, alkyl optionally substituted by aryl, alkoxy optionally substituted by aryl, aryl, CN, optionally substituted alkoxy, optionally substituted aryloxy, optionally substitute alkanoyl, optionally substituted aroyl, NO2, NR30R31, in which R30 and R31, which may be the same or different, represent hydrogen, optionally substituted alkyl or optionally substituted aryl; additionally, one of R30 and R31 may represent optionally substituted alkanoyl or optionally substituted aroyl, n represents an integer from 0 to 2, in addition, when an adjacent pair of A1 - A4 each represent CR1, then the adjacent carbon atoms, together with their substituents may form a ring B, when X is CR6R7, R6 and R7, together with the carbon atom to which they are attached may form a ring C, or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the therapeutic and/or prophylactic treatment of Duchenne muscular dystrophy, Becker muscular dystrophy or cachexia.
Synthesis of 2-arylbenzoxazoles via DDQ promoted oxidative cyclization of phenolic Schiff bases - A solution-phase strategy for library synthesis
Chang, Junbiao,Zhao, Kang,Pan, Shifeng
, p. 951 - 954 (2007/10/03)
The Schiff base derived from the condensation of o-aminophenol with benzaldehydes was induced to undergo oxidative cyclization in the presence of DDQ. The resulting 2-arylbenzoxazoles were separated from the reduced DDQ by product by treatment of reaction mixture with a strongly basic ion-exchange resin. The applicability of this chemistry to spatially separate library synthesis is demonstrated by the preparation of a 352-member library.
