European Journal of Medicinal Chemistry p. 201 - 207 (1998)
Update date:2022-09-26
Topics:
Dumoulin, Hugues
Boulouard, Michel
Daoust, Martine
Rault, Sylvain
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.
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