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- W2187942122 abstract "Benzodiazepines are widely used in neurological disorders. Binding benzodiazepine to specific GABA receptor domain increases frequency of opening the chloride channel results in pharmacological effects of benzodiazepines that leads to effects such as anti-anxiety, sleeping, anticonvulsant and muscle relaxant. To achieve compounds as a benzodiazepine agonist with more selective effects on benzodiazepine receptors, on basis of structure-activity relationship (SAR) of Benzodiazepine receptor ligands, some new derivatives of 4-amino-3,5-diphenyl-1,2,4-triazole were developed. 3,5-diphenyl 1,2,4-triazole was synthesized by the reaction of the benzonitrile with hydrazine hydrate subsequent was chlorinated in the presence of chloroacetyl chloride. Final products were obtained by the treatment of the latter intermediate with various amines. Based on the structure-activity relationship (SAR), derivatives of 3,5-diphenyl 1,2,4-triazole as benzodiazepine receptor agonists were designed. Molecular modeling studies indicated that the pharmacophore groups of the designed compounds and estazolam (potent benzodiazepine agonist) were well matched. The designed structures were synthesized in acceptable yield and their structures were approved using instrumental methods including Mass spectrometry and NMR spectroscopy. In this study, 3,5-diphenyl-4H-1,2,4-triazol-4-amine derivatives were designed and synthesized as GABA receptor selective agonists. Since molecular modeling studies showed favorable results, we could expect appropriate pharmacological effects of the novel compounds. Keyword: Synthesis. benzodiazepine. ligand. triazole" @default.
- W2187942122 created "2016-06-24" @default.
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- W2187942122 date "2014-01-01" @default.
- W2187942122 modified "2023-09-24" @default.
- W2187942122 title "Design and synthesis of 3,5-diphenyl-4H-1,2,4-triazol-4-amine derivatives as novel benzodiazepine receptor ligands" @default.
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