2-OXO-2-(PHEN-2-YLPYRROL-2-YL)ACETAMIDES AS POTENTIAL ANXIOLYTIC AGENTS - SYNTHESIS AND AFFINITY AT THE CENTRAL BENZODIAZEPINE RECEPTOR

A series N-substituted 2-hydroxy and 2-oxo-2-(phen-1-ylpyrrol-2-yl)ace tamides were synthesized and their affinity at the benzodiazepine rece ptor tested. Isosteric replacement of the indolyl ring in previously d escribed derivatives by a phen-1-ylpyrrole led to the synthesis of sev en compounds 8-9, 12-14, 23 and 26 with benzodiazepine affinity (K-1 l ess than or equal to 0.90 mu M). Among these, 26 exhibits an interesti ng anxiolytic activity and weak lateral effects. (C) Elsevier, Paris.