2-Oxo-2-(phen-2-ylpyrrol-2-yl)acetamides as potential anxiolytic agents: Synthesis and affinity at the central benzodiazepine receptor

Article abstract of DOI:10.1016/S0223-5234(98)80009-3

A series of N-substituted 2-hydroxy and 2-oxo-2-(phen-1-ylpyrrol-2-yl)acetamides were synthesized and their affinity at the benzodiazepine receptor tested. Isosteric replacement of the indolyl ring in previously described derivatives by a phen-1-ylpyrrole led to the synthesis of seven compounds 8-9, 12-14, 23 and 26 with benzodiazepine affinity (K(i) ≤ 0.90 μM). Among these, 26 exhibits an interesting anxiolytic activity and weak lateral effects.