Anticonvulsant activity of 7-phenyl-5H-thiazolo[5,4-e][1,2,3,4]tetrazolo[5,1-c]pyrrolo[1,2-a][1,4]diazepine (5) and 7-phenyl-5H-thiazolo[5,4-e][1,3,4]triazolo[5,1-c]pyrrolo[1,2-a][1,4]diazepines (6a-d) was measured against pentylenetetrazole (PTZ)-induced seizures in mice. Intraperitoneal injections of different doses (12.5, 25 and 50 mg/kg, i.p.) of test compounds decreased PTZ-induced seizure...

The title compound, C(17)H(18)N(2)O(4), is the methyl ester of the adduct of intra-molecular Diels-Alder reaction between maleic anhydride and 1-(2-fur-yl)-2,3,4,5-tetra-hydro-1H-pyrrolo-[1,2-a][1,4]diazepine. The mol-ecule comprises a fused penta-cyclic system containing four five-membered rings (viz. pyrrole, 2-pyrrolidinone, tetra-hydro-furan and dihydro-furan) and one seven-membered ring (1...

A compound that is involved in the biosynthesis of the drosopterin eye pigments has been isolated from the heads of Drosophila melanogaster. Analyses of this compound by chemical, mass spectral, and proton nuclear magnetic resonance techniques in conjunction with biochemical considerations provide evidence for the structure 2-amino-4-oxo-6-acetyl-7,8-dihydro-3H,9H-pyrimido[4,5-b][1,4]diazepine ...

In the present paper, we report on the synthesis, and in vitro antiviral and cytostatic activities of a series of novel imidazole[4,5-e][1,3]diazepine-4,8-dione (compounds 9-11) and acyclic carbamoyl imino-ureido imidazole (compounds 12 and 13) derivatives. These new type of chemical entities showed no significant activity on the broad spectrum of DNA and RNA viruses. Results of antiproliferati...

A series of morpholine substituted amino acids (phenylalanine, leucine, lysine and glutamic acid) was synthesized. A fragment-based screening approach was then used to evaluate a series of small heterocycles, including morpholine, oxazoline, dihydro-1,3-oxazine, tetrahydro-1,3-oxazepine, thiazoline, tetrahydro-1,3-pyrimidine, tetrahydro-1,3-diazepine and hexahydro-1H-benzimidazole, as potential...

Piperazines are found widely in commercially-available compounds and bioactive molecules (including many drugs). However, in the vast majority of these molecules, the piperazine ring is isolated (i.e. not fused to another ring) and is not substituted on any of its carbon atoms. A modular synthetic approach is described in which combinations of cyclic sulfamidate and hydroxy sulfonamide building...

W. S. H am am a Chemistry D epartm ent, Faculty of Science, M ansoura University, M ansoura, Egypt R eprint requests to Dr. W. S. H am am a. E-mail: Sinfac@ mum.mans.eun.eg Z. Naturforsch. 55b, 443-447 (2000); received January 25, 2000 6-Am inouracil, M annich Reaction, Pyrimido[4,5-d]pyrim idine The reaction of 6-am inouracil 1 with form aldehyde and secondary amines in ethanol at room tem per...

A new series of tetrahydro-quinazoline and tetrahydro-1H-dibenzo[b,e][1,4]diazepine analogs were synthesized and tested for their DHFR inhibition and in vitro antitumor activity. Compound 35 showed a remarkable DHFR inhibitory potency (IC₅₀, 0.004 μM) which is twenty fold more active than methotrexate (MTX). Compounds 17 and 23 proved to be fifteen fold more active than the known antitumor 5-FU...

The DATA chelators, are a novel class of tri-anionic chelators ligands based on the 6-amino1,4-diazepine-triacetic acid, core structure, that have been introduced recently for the chelation of Ga. Compared to established macrocyclic chelators based on the cyclen scaffold (i.e. DOTA-, DO3Aand DO2Aderivatives), they enable undergo quantitative radiolabelling both more rapidly and under considerab...

A new 1,4-diazepine, callysponine (1), was isolated from a South China Sea Callyspongia sp. marine sponge, together with four known proline-based diketopiperazines: cyclo-(S-Pro-R-Leu) (2), cyclo-(S-Pro-R-Val) (3), cyclo-(S-Pro-R-Ala) (4), andcyclo-(S-Pro-R-Tyr) (5). The new structure was determined on the basis of NMR and MS analysis, and the absolute stereochemistry was defined by NOESY spect...