| Literature DB >> 30773432 |
Dominique Lesuisse1, André Malanda2, Jean-François Peyronel2, Yannick Evanno2, Patrick Lardenois2, Danielle De-Peretti2, Pierre-Yves Abécassis3, Pascal Barnéoud4, Pascale Brunel5, Marie-Claude Burgevin6, Céline Cegarra4, Florian Auger2, Amélie Dommergue2, Corinne Lafon7, Luc Even2, Joanna Tsi2, Thy Phuong Hieu Luc2, Antonio Almario2, Anne Olivier6, Marie-Noëlle Castel8, Véronique Taupin4, Thomas Rooney4, Xavier Vigé6.
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.Entities:
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Year: 2019 PMID： 30773432 DOI： 10.1016/j.bmcl.2019.01.024
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823