Neuropharmacological screening of two 1,5-benzodiazepine compounds in mice

Crystallographic and first‐principles density functional theory study on the structure, noncovalent interactions, and chemical reactivity of 1,5‐benzodiazepin‐2‐ones derivatives

“…Besides their significant medicinal and pharmacological applications, containing 1,5‐benzodiazepines derivatives, have also been reported to exhibit noteworthy photophysical properties . In this context, Hasan and coworkers (our collaborators in present work) were previously performing the preparation of photoluminescent material 4‐(2′‐hydroxyphenyl)‐1,5‐benzodiazepin‐2‐one compound 1, which manifested very interesting anticonvulsant and hypnotic activities . Indeed, obtained compound has been used to design two fluorogenic probes for the selective detection of biothiols .…”

“…The mean planes of the diazepine ring are twisted with respect to that of the benzene ring by 19.95(7) and 25.02(9) in 1 and 2, respectively. The Cremer-Pople puckering parameters are [42] -compound 1: q 2 = 0.7902 (14) Å, q 3 = 0.2560 (15) Å, φ 2 = 28.17 (11) , φ 3 = 127.0 (3) , and Q = 0.8306 (15) Å; compound 2: q 2 = 0.8400 (18) Å, q 3 = 0.2297 (19) Å, φ 2 = 210.14 (13) , φ 3 = 305.8 (5) , and Q = 0.8707 (19). The dihedral angles between the C1-C6 benzene ring planes and those formed by C8-C13 phenol ring (in 1) and C8-C13 phenylacetate ring system (in 2) are 41.60 (8) and 18.37 (10) ( Figure S1).…”

“…1, which manifested very interesting anticonvulsant and hypnotic activities. [9,11] Indeed, obtained compound has been used to design two fluorogenic probes for the selective detection of biothiols. [9] From a structural point of view, it seems that compound 1 establishes strong intramolecular and intermolecular O-H…N and N-H…O hydrogen bonds.…”

(4Z)-4-(2-Oxopropylidene)-1,3-bis(prop-2-en-1-yl)-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-2-one

“…1,5-Benzodiazepine derivatives have attracted much attention as they exhibit pronounced anxiolytic, sedative, hypnotic and anticonvulsant activities with low toxicity (Landquist et al, 1984;Hamor et al, 1984;Ben-Cherif et al, 2010). They are also used as an intermediates for the synthesis of new heterocyclic systems (Ahabchane et al, 2001;Minnih et al, 2014).…”

(4E)-1-Decyl-4-(2-oxopropylidene)-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-2-one

“…1,5-Benzodiazepine derivatives constitute an important class of nitrogen-containing heterocycles and possess interesting activities as anticonvulsant (Ben-Cherif et al, 2010), antimicrobial (Wang et al, 2015), and anti-inflammatory (Ha et al, 2010) agents. They have also been used as intermediates for the synthesis of benzimidazoles (El Azzaoui et al, 1999) and quinoxalines (Doumbia et al, 2008).…”