1,721,013 research outputs found
8-Azapurine nucleus: a versatile scaffold for different targets
No full text8-Azapurine nucleus is a bioisoster of the purine nucleus. Variously substituted 8-azapurines have been synthesised and studied for their interactions with many enzymes and receptors and for their antitumor and antiviral activity. In this paper the main results of the studies made in these last years
on this topic are reported
N(9)-substituted 2-phenyl-N(6)-benzyl-8-azaadenines: A1 adenosine receptor affinity. A comparison with the corresponding N(6)-substituted 2-phenyl-N(9)-benzyl-8-azaadenines
No full textThe synthesis and the assay of title compounds were accomplished. Biological results indicated the general lack of activity among the tested disubstituted compounds hearing the benzyl group on N(6) and confirmed the activity of those with this group on N(9)
1,2,3 Triazolo[1,2-a]benzotriazoles or 2,3-Benzo-1,3a,6,6a-Tetraazapentalenes
No full textSome new v-triazolo[1,2-a]benzotriazoles or 2,3-benzo-1,3a,6,6a-tetraazapentalenes were prepared according to previously employed synthetic routes concerning deoxycyclization reactions of appropriate nitrophenyl-1,2,3-triazole derivatives and/or thermal decompositions of appropriate azidophenyl-1,2,3-triazoles. The nitration of 9-phenyl-1,2,3-triazolo[1,2-a]benzotriazoles allowed the isolation of some mononitro- and trinitro-derivatives, whose structures were assigned by chemical and spectroscopic methods
"One Pot" Synthesis of 2-Substituted 9-(2'-Hydroxy-3'-aminopropyl)-8-azahypoxanthines and 8-Azaadenines [5-Substituted 3-(2'-Hydroxy-3'-aminopropyl)-7-amino and 7-hyroxy- 3H-1,2,3-triazolo[4,5-d]pyrimidines]
No full textAn example of the generalization of the synthesis of 8-azahypoxanthines A and 8-azaadenines B, interesting from a medicinal point of view, is presented by utilizing 1-amino-2-hydroxy-3-azidopropanes
Modification of the 1,2,3-Triazole Ring Present in an Effective in vitro Inhibitor of Prostaglandin Synthesis
No full text1,2,3-Triazolo[4,5-d]-1,2,4-triazolo[4,3-b]pyridazines
No full textSome new 1,2,3-triazolo[4,5-d]-1,2,4-triazolo[4,3-b]pyridazines were prepared starting from the corresponding 1,2,3-triazolo[4,5-d]pyridazines via the formation of the 1,2,4-triazole ring, by condensation of an appropriate monocarbon fragment with the 4-hydrazino substituent and the nitrogen atom in the 5 position of the heterocycle. Condensation of 4-phenylhydrazino substituted derivatives with formic acid gave zwitterionic compounds
In vitro Inhibitors of Prostaglandin Synthesis: (p-Thiosubstituted)-Benzyl Nitrogen Heterocycles
No full textXanthine Oxidase (XO). Synthesis of 4(5)-Carbxyamido-5(4)-aminoalkanoyl)amino-1,2,3-triazoles and Their Cyclization to 8-Azahypoxanthines. Evaluation for Inhibition of XO.
No full textSynthesis of hypoxanthine and triazole derivatives by reaction of 4(5)-amino-5(4)-carboxyamido-1,2,3-triazole with protected aminoacids are reported. The synthesized compounds had no inhibitory activity on Xanthine Oxidase
Synthesis of New 3-Benzyl-5-Phenyl-7-Alkylaminothiazolo[4,5-d]pyrimidine-2(3H)-Thiones.)
No full textThis paper describes the preparation of title compounds starting from 3-benzyl-4-amino-5-carboxyamidothiazole-2(3H)-thione, which, by heating with alkyl orthobenzoates, was converted into 3-benzyl-5-phenyl-7-alkoxy-thiazolo[4,5-d]pyrimidines. The treatment of these compounds with hydrobromic acid in acetic acid gave 3-benzyl-5-phenyl-7-oxo-thiazolo[4,5-d]pyrimidine-2(3H)-thione which, by reaction with phosphorus oxychloride and subsequent substitution of the halogen with amines, gave the corresponding title compounds
Synthesis of 4,6-disubstituted- and 4,5,6-trisubstituted-2-phenyl-pyrimidines and their affinity towards A(1) adenosine receptors
No full textSynthesis and assay of title compounds are reported. The results can support our hypothesis about the possibility that molecules characterized by great flexibility, as the title 2-phenyl-4,5,6-triaminopyrimidines, can better interact with the receptor sites compared with rigid molecules as 2,6,9-trisubstituted 8-azaadenines. Relatively low activity shown by pyrimidine derivatives demonstrated the importance of the bicyclic aromatic system in 8-azaadenines and adenines to give a favourable interaction between a hexogenous molecule and the A(?)1 adenosine receptors
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