939820-82-3Relevant academic research and scientific papers
From pyrroles to 1-oxo-2,3,4,9-tetrahydro-1H-β-carbolines: A new class of orally bioavailable mGluR1 antagonists
Fabio, Romano Di,Micheli, Fabrizio,Alvaro, Giuseppe,Cavanni, Paolo,Donati, Daniele,Gagliardi, Tatiana,Fontana, Gabriele,Giovannini, Riccardo,Maffeis, Micaela,Mingardi, Anna,Tranquillini, Maria Elvira,Vitulli, Giovanni
, p. 2254 - 2259 (2007)
Exploiting the SAR of the known pyrrole derivatives, a new class of mGluR1 antagonists was designed by replacement of the pyrrole core with an indole scaffold and consequent cyclization of the C-2 position into a tricyclic β-carboline template. The appropriate exploration of the position C-6 with a combination of H-bond acceptor groups coupled with bulky/lipophilic moieties led to the discovery of a new series of mGluR1 antagonists. These compounds exhibited a non-competitive behavior, excellent pharmacokinetic properties, and good in vivo activity in animal models of acute and chronic pain, after oral administration.
