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Updated: Jun 7, 2026

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
Synthesis of disubstituted 1,4-diazepines with affinity to GABAA-receptor subtypes
D Briel1, I Rudolph, K Unverferth
1Institute of Pharmacy, University of Leipzig, Germany. briel@rz.uni-leipzig.de
Abstract:
A series of tetrahydro-1 H-1,4-diazepines 4a-c, dihydro-1 H-1,4-diazepine 5 and pyrido diazepines 8 and 10 was prepared. Originated form dehydroacetic acid (DHA) and aromatic aldehydes cinnamoyl compounds 3a-c were obtained and converted with ethylenediamine to give tetrahydro-1H-1,4-diazepines 4a-c. For the synthesis of pyrido[1,2-d][1,4]diazepines 8 and 10 a new snythetic approach is described. Compounds 4b and 5 were investigated concerning their affinity to different benzodiazepine receptor subtypes. The determined IC50 values for 5 are 1.5 microM and 1.1 microM at 10 microM respectively.
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