Imidazobenzodiazepines - an overview | ScienceDirect Topics
Mar 3, 2012 · Imidazole-fused benzodiazepines are prominent pharmacophores proved to be potent central nervous system (CNS) depressants in several marketed drugs such as loprazolam, flumazenil, and midazolam (Welsch et al., 2010). Considering this background, the development of simple and efficient platforms to construct new imidazole-fused benzodiazepines ...
Chemical structure and properties of midazolam compared with …
2 Some properties of midazolam that are of special interest for its practical use are discussed, such as: the basicity of its imidazole ring nitrogen, which allows water-soluble salts and well-tolerated aqueous injectable solutions to be prepared; its stability to hydrolytic degradation; its rapid metabolic inactivation, which is mainly ...
Imidazobenzodiazepines - an overview | ScienceDirect Topics
Imidazobenzodiazepines are a type of benzodiazepine site ligands that interact with specific receptor subtypes in the brain, such as α4βγ2 or α6βγ2 receptors, and are used for identification purposes in neuroscience research. AI generated definition based on: Neuropharmacology, 2009
Benzodiazepines | Anesthesiology Core Review: Part One Basic …
The most common intravenous benzodiazepines administered in the perioperative setting are midazolam, diazepam, and lorazepam. Benzodiazepines produce hypnosis, sedation, anxiolysis, anterograde amnesia, anticonvulsion, and centrally produced muscle relaxation. They do not provide any analgesia.
Midazolam (Versed, Roche, U.S.A.; Dormicum, Roche, other countries; Ro 21 -3981) is the first ben- zodiazepine derivative with water-soluble salts. It represents an advance in drug efficacy and safety in the treatment of insomnia and as the sedative-hyp- …
1,4-Benzodiazepines: Chemical stability and ... - ScienceDirect
Dec 1, 2021 · The incorporation of imidazole or triazole at 1, 2 position of benzodiazepine can increase the stability of the drug such as alprazolam, midazolam and estazolam [9]. Different from the common benzodiazepines, flumazenil is clinically used as GABA receptor antagonist since it does not have a benzene substituted imine (Fig. 1).
Benzodiazepines - SpringerLink
Aug 14, 2020 · Currently, approximately 24 benzodiazepines, including prodrugs, are approved for use in the United States and are prescribed as anxiolytics, muscle relaxants, anesthetic adjuncts, anticonvulsants, and treatment for obsessive-compulsive disorders. The properties of selected benzodiazepines are summarized in Table 20.1.
Chromatographic separation of the interconverting enantiomers of ...
Jun 21, 2021 · A structural variation of the classical benzodiazepine skeleton is observed e.g. in alprazolam, midazolam, and related benzodiazepines, which contain a 1,2,4-triazole or an imidazole ring fused to the benzodiazepine core.
Unexpected transformation of 1,5-benzodiazepine derivatives …
Jun 24, 2023 · In an attempt to synthesize new derivatives of imidazo[1,5-a][1,5]benzodiazepine-3-carboxylic acid esters by activation of the amide group of the heterocycle to iminophosphate and its cyclocondensation with ethyl isocyanoacetate, unexpected 5-substituted ethyl oxazole-4-carboxylates were obtained as the main products.
Synthesis and evaluation of imidazo[1,5-a][1,4]benzodiazepine …
Apr 1, 1993 · Quantitative Structure–Activity Relationship Studies for the Binding Affinities of Imidazobenzodiazepines for the α6 Benzodiazepine Receptor Isoform Utilizing Optimized Blockwise Variable Combination by Particle Swarm Optimization for …