Development of a novel NURR1/NOT agonist from hit to lead and candidate for the potential treatment of Parkinson's disease. Issue 7 (1st April 2019)

• Record Type: Journal Article
• Authors: Lesuisse, Dominique; Malanda, André; Peyronel, Jean-François; Evanno, Yannick; Lardenois, Patrick; De-Peretti, Danielle; Abécassis, Pierre-Yves; Barnéoud, Pascal; Brunel, Pascale; Burgevin, Marie-Claude; Cegarra, Céline; Auger, Florian; Dommergue, Amélie; Lafon, Corinne; Even, Luc; Tsi, Joanna; Luc, Thy Phuong Hieu; Almario, Antonio; Olivier, Anne; Castel, Marie-Noëlle; Taupin, Véronique; Rooney, Thomas; Vigé, Xavier
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 29:Issue 7(2019)
• Page Start: 929
• Page End: 932
• Publication Date: 2019-04-01
• Subjects: Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2019.01.024
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: 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.