Discovery and lead optimisation of a potent, selective and orally bioavailable RARβ agonist for the potential treatment of nerve injury

Oxadiazole replacement of an amide linkage in an RARα agonist template 1, followed by lead optimisation, has produced a highly potent and selective RARβ agonist 4-(5-(4,7-dimethylbenzofuran-2-yl)-1,2,4-oxadiazol-3-yl)benzoic acid (10) with good oral bioavailability in the rat and dog. This molecule...

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Publicado en:Bioorg Med Chem Lett
Main Authors: Goncalves, Maria B., Clarke, Earl, Jarvis, Christopher I., Barret Kalindjian, S., Pitcher, Thomas, Grist, John, Hobbs, Carl, Carlstedt, Thomas, Jack, Julian, Brown, Jane T., Mills, Mark, Mumford, Peter, Borthwick, Alan D., Corcoran, Jonathan P.T.
Formato: Artigo
Idioma:Inglês
Publicado: Elsevier Science Ltd 2019
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Article
Acceso en liña:https://ncbi.nlm.nih.gov/pmc/articles/PMC6419571/
https://ncbi.nlm.nih.gov/pubmed/30792038
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2019.02.011
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