From pyrroles to 1-oxo-2, 3, 4, 9-tetrahydro-1H-β-carbolines: A new class of orally bioavailable mGluR1 antagonists

…, D Donati, T Gagliardi, G Fontana, R Giovannini…

Index: 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 Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 8 p. 2254 - 2259

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Citation Number: 33

Abstract

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. ...