Discovery of 2-arylbenzoxazoles as upregulators of utrophin production for the treatment of Duchenne muscular dystrophy

…, PD Johnson, AG Lambert, D Lawrence…

Index: 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, Severine 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. Journal of Medicinal Chemistry, 2011 , vol. 54, # 9 p. 3241 - 3250

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Citation Number: 32

Abstract

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 ...