Development of a novel NURR1/NOT agonist from hit to lead and candidate for the potential treatment of Parkinson's disease.
Bioorganic & Medicinal Chemistry Letters(2019)
摘要
In the course of a programme aimed at identifying Nurr1/NOT agonists for potential treatment of Parkinson’s disease, a few hits from high throughput screening were identified and characterized. A combined optimization pointed to a very narrow and stringent structure activity relationship. A comprehensive program of optimization led to a potent and safe candidate drug displaying neuroprotective and anti-inflammatory activity in several in vitro and in vivo models.
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关键词
novel nurr1/not,parkinson
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