Author/Authors :
Alfonzo D. Jordan، نويسنده , , Anil H. Vaidya، نويسنده , , Daniel I. Rosenthal، نويسنده , , Barry Dubinsky، نويسنده , , Cheryl P. Kordik، نويسنده , , Pauline J. Sanfilippo and، نويسنده , , Wu-Nan Wu، نويسنده , , Allen B. Reitz، نويسنده ,
Abstract :
A series of pyrido[1,2-a]benzimidazoles (PBIs) with substitution on the N5-nitrogen has been synthesized and found to possess high affinity for the benzodiazepine (BZD) site on the GABA-A receptor. The compounds evaluated include those bearing a heteroalkyl group and heterocyclic rings. The most promising of these compounds is ethoxymethyl analogue 24, which has an IC50 of 0.1 nM for the BZD site on the GABA-A receptor and has been advanced to human clinical trials.
