Synthesis, pharmacology and molecular modeling of N-substituted 2-phenyl-indoles and benzimidazoles as potent GABA A agonists

…, M González, I Buira, E Méndez, J Terencio…

Index: Falco, Jose Luis; Pique, Maria; Gonzalez, Miguel; Buira, Irma; Mendez, Eva; Terencio, Jose; Perez, Cristina; Princep, Marta; Palomer, Albert; Guglietta, Antonio European Journal of Medicinal Chemistry, 2006 , vol. 41, # 8 p. 985 - 990

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Citation Number: 44

Abstract

Among the known non-benzodiazepine hypnotic drugs, Zolpidem (1a), Indiplon (2a) and Zaleplon (2b) have shown high affinity and selectivity for the α1 subunit of the GABA-A receptor. Our group has performed pharmacophoric and ADMET-prediction studies to evaluate a virtual library of new molecules based on privileged structures. Among these, we have synthesized a library of N-substituted indoles and a library of N-substituted ...