Discovery and SAR of 2-arylbenzotriazoles and 2-arylindazoles as potential treatments for Duchenne muscular dystrophy

Olivier De Moor; Colin R Dorgan; Peter D Johnson; Adam G Lambert; Cristina Lecci; Carole Maillol; Gary Nugent; Séverine D Poignant; Paul D Price; Richard J Pye; Richard Storer; Jonathon M Tinsley; Richard Vickers; Renate van Well; Fraser J Wilkes; Francis X Wilson; Stephen P Wren; Graham M Wynne

doi:10.1016/j.bmcl.2011.06.047

Discovery and SAR of 2-arylbenzotriazoles and 2-arylindazoles as potential treatments for Duchenne muscular dystrophy

Bioorg Med Chem Lett. 2011 Aug 15;21(16):4828-31. doi: 10.1016/j.bmcl.2011.06.047. Epub 2011 Jun 17.

Authors

Olivier De Moor¹, Colin R Dorgan, Peter D Johnson, Adam G Lambert, Cristina Lecci, Carole Maillol, Gary Nugent, Séverine D Poignant, Paul D Price, Richard J Pye, Richard Storer, Jonathon M Tinsley, Richard Vickers, Renate van Well, Fraser J Wilkes, Francis X Wilson, Stephen P Wren, Graham M Wynne

Affiliation

¹ Summit plc., 91 Milton Park, Abingdon, Oxfordshire OX14 4RY, United Kingdom.

PMID: 21741236
DOI: 10.1016/j.bmcl.2011.06.047

Abstract

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.

MeSH terms

Dose-Response Relationship, Drug
Drug Discovery*
Humans
Indazoles / chemical synthesis*
Indazoles / chemistry
Indazoles / therapeutic use
Microsomes, Liver / drug effects*
Molecular Structure
Muscular Dystrophy, Duchenne / drug therapy
Solubility
Stereoisomerism
Structure-Activity Relationship
Triazoles / chemical synthesis*
Triazoles / chemistry
Triazoles / therapeutic use

Substances

Indazoles
Triazoles
benzotriazole