1,4-Diazepines

Synthesis and Chemistry of Benzo[e][1,2,6]thiadiazino[3,4-b][1,4]diazepin-10(11H)-ones and Related Ring Transformations

“…Benzo­[ e ]­[1,4]­diazepines and their hetareno-fused analogues can act as allosteric enhancers of the binding of the neurotransmitter gamma-amino butyric acid (GABA) in the neuronal GABA A receptors . This behavior has led to uses in pharmaceuticals, in particular, as psychoactive drugs with anxiolytic, sedative, and hypnotic activity, e.g., commercial 1,4-benzodiazepine drugs include diazepam (anxiolytic) and flumazenil (benzodiazepine overdose antidote) (Figure ).…”

Enol-imino–Keto-enamine Tautomerism in a Diazepine Derivative: How Decisive Are the Intermolecular Interactions in the Equilibrium?

“…Diazepines (DZPs) constitute the main pharmacologically active compounds with different applications in medicinal chemistry. 1,4-Diazepine heterocycles such as the well-known zometapine, etizolam, brotizolam, clozapine, dibenzepine, and diazepam − cover a wide range of biological activities. Some 1,4-benzodiazepine derivatives were found to be active in the treatment of insomnia, epilepsy, and alcoholism .…”

A facile access to new diazepines derivatives: Spectral characterization and crystal structures of 7-(thiophene-2-yl)-5-(trifluoromethyl)-2,3-dihydro-1 H -1,4-diazepine and 2-thiophene-4-trifluoromethyl-1,5-benzodiazepine

“…2 (1) (117.94(19)°) bond lengths and angle, respectively, are similar to those measured for other structurally characterized trifluoroacetyl-containing organic compounds [32,33]. 110.2 (2). Symmetry transformations used to generate equivalent atoms: #1 -x, -y, -z.…”

“…Diazepines are found in various psychoactive pharmaceutical drugs, v. g. diazepam [1], and specifically as 1,4-diazepines [2]. Meanwhile, benzodiazepines have been thoroughly studied during a period of several decades, largely because of their relatively easy synthesis from common starting materials [3], and they have become of ever-increasing interest to investigators, inasmuch as their pharmacological activities (tranquilizers, substances that lower blood pressure, analgesics and sedative agents) [3].…”