Synthesis of pyrimido[1,4]diazepin-2-one analogs and their evaluation as anticonvulsant agents

Synthesis, crystal structure and computational analysis of 2,7-bis(4-chlorophenyl)-3,3-dimethyl-1,4-diazepan-5-one

“…Quite a few reports have long established that 1,4-diazepane derivatives (Sethuvasan et al, 2016;Maheshwaran et al, 2015) are chemically (Baliah et al, 1978;Thennarasu & Perumal, 2002) and biologically (Murthy & Knaus, 1999;Wolkinger et al, 2009) significant motifs. In the view of widespread applications of 1,4-diazepane in the synthetic and medicinal fields, we report here the synthesis, crystal structure and computational analysis of 2,7-bis(4-chlorophenyl)-3,3-dimethyl-1,4diazepan-5-one (I).…”

Synthesis of (7S)-(−)-7-aryl-5-methyl-7-trifluoromethyl-1,3,6,7-tetrahydro-2H-1,4-diazepin-2-ones

“…Some 1,4-diazepine derivatives were found to act as effective lymphocyte function-associated antigen-1 (LFA-1) antagonists [1,2] (LFA-1 plays a critical role in leukocyte adhesion to and migration through endothelium by its ability to bind intercellular adhesion molecules), which considerably affects pathogenesis of many diseases [3,4]. Some 1,4-diazepines also displayed anticonvulsant activity [5]. Furthermore, 1,4-diazepine ring constitutes a structural fragment of nucleoside antibiotic liposidomycin B [6] which inhibits bacterial synthesis of peptidoglycan [7].…”

A novel, microwave-assisted method for the synthesis of alicyclic-condensed 5H-1,4,6,7-tetrahydro-1,4-diazepin-5-ones

“…To the best of our knowledge, there has been only one report on the synthesis of cycloalkanecondensed 1,4-diazepinones. 1 However, certain 1,4-diazepin-5-ones exhibit significant biological properties, for example, as lymphocyte function-associated antigen-1 inhibitors, 2 anticonvulsants, 3 HIV-1 reverse transcriptase inhibitors, 4 pharmacophores for structure-activity relationships, 5 and most recently, c-turn-like mimics. 6 We report here an efficient, microwave (MW)-assisted method for the preparation of cis-and trans-cyclohexane-and cis-cyclopentane-condensed 5H-1,4,6,7-tetrahydro-1,4-diazepin-5-ones.…”