Corrigendum to “Discovery and lead optimisation of a potent, selective and orally bioavailable RARβ agonist for the potential treatment of nerve injury” [Bioorg. Med. Chem. Lett. 29(8) (2019) 995–1000]

Bioorganic & Medicinal Chemistry Letters(2019)

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摘要
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 increases neurite outgrowth in vitro and induces sensory axon regrowth in vivo in a rodent model of avulsion and crush injury, and thus has the potential for the treatment of nerve injury.
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关键词
Retinoic acid receptor,Beta agonist,SAR,Neurite outgrowth,Axon regrowth,C286
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