The enzyme system responsible for the conversion of 2-amino-4-oxo-6-(D-erythro-1',2',3'-trihydroxypropyl)-7,8-dihyd roptridine triphosphate (dihydroneopterin triphosphate or H2-NTP) to 2-amino-4-oxo-6-acetyl-7,8-dihydro-3H,9H-pyrimido[4,5-b]-[1,4]diazepine (pyrimidodiazepine or PDA), a precursor to the red eye pigments, he drosopterins, has been purified from the heads of Drosophila melanogaste...

was positive but the rest of tested benzodiazepines were negative. Previous reports2 suggest that there is no cross-reactivity among benzodiazepines. Diazepam is the most similar benzodiazepine to tetrazepam, the only difference between them is the presence at position 5 on the diazepine ring of phenyl in diazepam and clohexen in tetrazepam, and this cyclohexene conformation could explain tetra...

Imidazo[1,5-a][1,4]benzodiazepines are well documented to exhibit potent activity at GABAA/Bz receptors. This series belongs to one of the very few chemical families, which have been extensively investigated for GABAA/Bz receptor mediated activity.1,2 Flumazenil (Ro 15-1788), an imidazo[1,5-a][1,4]benzodiazepine, was earlier shown to bind to central GABAA receptors with little or no intrinsic a...

Synthetic approaches are reported to polydentate ligands based on 6-phenyl-6-amino-perhydro-1,4-diazepine. The synthetic route devised averts ring-opening reactions, allowing the exocyclic N-substituent to be introduced separately and involves a nitro-Mannich condensation, prior to chemoselective RANEY® nickel reduction. Comparison of the solid-state structures of four synthetic intermediates r...

We describe new synthetic routes developed toward a range of substituted analogues of bromo and extra-terminal (BET) bromodomain inhibitors I-BET762/JQ1 based on the triazolo-benzodiazepine scaffold. These new routes allow for the derivatization of the methoxyphenyl and chlorophenyl rings, in addition to the diazepine ternary center and the side chain methylene moiety. Substitution at the level...

A series of novel 1,4diazepines have been synthesized from β-diketones / β-ketoesters of 4acetylaminobenzene sulphonyl chloride. Desired compounds were prepared by the reaction of novel βdiketone / β-ketoester derivatives of [N4-(4acetylamino) benzene sulphonyl piperazinylN1-1bromopropane] with ethylenediamine to get 1, 4dizapines. All the newly synthesized compounds were characterized with IR ...

The compound 2-amino-4-oxo-6-acetyl-7,8-dihydro-3H,9H-pyrimido[4,5-b]-[1,4]diazepine (pyrimidodiazepine or PDA, for short) is a precursor of the red eye pigments called the drosopterins in Drosophila melanogaster. The precursor of PDA is 2-amino-4-oxo-6-(D-erythro-1',2',3'-trihydroxypropyl)-7,8-dihydrop teridine triphosphate (dihydroneopterin triphosphate or H2-NTP). The synthesis of of PDA fro...