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. 2019 Apr 1;29(7):929-932.
doi: 10.1016/j.bmcl.2019.01.024. Epub 2019 Jan 30.

Development of a novel NURR1/NOT agonist from hit to lead and candidate for the potential treatment of Parkinson's disease

Dominique Lesuisse  1 , André Malanda  2 , Jean-François Peyronel  2 , Yannick Evanno  2 , Patrick Lardenois  2 , Danielle De-Peretti  2 , Pierre-Yves Abécassis  3 , Pascal Barnéoud  4 , Pascale Brunel  5 , Marie-Claude Burgevin  6 , Céline Cegarra  4 , Florian Auger  2 , Amélie Dommergue  2 , Corinne Lafon  7 , Luc Even  2 , Joanna Tsi  2 , Thy Phuong Hieu Luc  2 , Antonio Almario  2 , Anne Olivier  6 , Marie-Noëlle Castel  8 , Véronique Taupin  4 , Thomas Rooney  4 , Xavier Vigé  6
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Development of a novel NURR1/NOT agonist from hit to lead and candidate for the potential treatment of Parkinson's disease

Dominique Lesuisse et al. Bioorg Med Chem Lett. .

Abstract

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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