In particular, among the triazoloquinazolines (1-11), the dialkoxy derivative (7b) was found to have the highest affinity at A 1 subtype receptor, and its radioligand binding activity together with 1,3-dipropyl-8-cyclopentylxanthine (DPCPX) was studied. Finally, the structure-activity relationship (SAR) studies on the titled compounds provide some new insights about steric hindrance and lipophilic requirements for anchoring to the adenosine receptors recognition site.

Synthesis and Properties of 3,6-Diamino-Substituted 1,2,4-Triazin-5(2H)-ones.-The ultrasound-promoted cyclocondensation of guanidines (I) with 2-amino--2-thioxoacetate (II) leads to the novel title triazinones (III) (7 examples). The acylation of the latter occurs regioselectively at ring position 2, presumably favoured by the formation of an intramolecular hydrogen bond. -(GEFFKEN*, D.; KOELLNER, M. A

2005Multi-membered N-heterocycles R 0690Oxalylation of N-Phenylanthranilic-O-alkylhydroxamates to 4-Alkoxy--2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-2,3,5-triones. -In the presence of imidazole as base, title products (III) are obtained as stable compounds. They represent the ring-enlarged analogues of antimicrobial agents of type (V). -(GEFFKEN*, D.; KOELLNER, M. A.; Z. Naturforsch., B: Chem. Sci. 60 (2005) 3, 337-340; Inst.

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Reaction of primary anthranilamide (I) with oxalyl chloride in the presence of imidazole gives selectively the title benzodiazepine (III) or benzoxazolodiazepine derivatives (IV) depending on the molar ratio of the reactants.