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Guida Pratica al riconoscimento delle sostanze iscritte nella X edizione della Farmacopea ufficiale della Repubblica Italiana
No full text1-(4-SUBSTITUTED-BENZYL)-1,2,3-TRIAZOLES, INVITRO INHIBITORS OF PROSTAGLANDIN SYNTHESIS
No full textNew 4-(4-phenylsubstituted)-1,2,3-triazolacetic acid derivatives of general formula (I) were prepared by nucleophilic substitution, 1,3-dipolar cycloaddition and functional group interconversion reactions. These compounds were evaluated as in vitro prostaglandin synthesis inhibitors. Only the isomeric compounds (II c) and (III e), with a 4-aminophenyl substituent on the triazole ring, inhibit arachidonic acid-induced malondialdehyde formation in human platelets; (II c) and (III e) are as effective as aspirin
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
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
EFFECTS OF SUBSTITUTED 1,2,3-TRIAZOLES ON ADENOSINE-DEAMINASE, GUANINE DEAMINASE AND XANTHINE-OXIDASE
No full textThe action of some known and new synthesized substituted 1,2,3-triazoles on adenosine deaminase, guanine deaminase and xanthine oxidase was studied. The effect of substituents in 1, 4 and 5 positions was studied and discussed. The presence of a carboxamido group in 4 position seems to be essential in the binding to adenosine deaminase
A Method for the Synthesis of Racemic and Optically Active 2-Substituted 9-(2',3'-Dihidroxypropyl)-8-Azahypoxanthines and 8-Azaadenines
No full textEvaluation of the Quantitative Contribution of a Phenyl Group on C(2) of 8-Azaadenosine to the Binding with Adenosine Deaminase: a New Synthesis of 8-Azaadenosine. XI.
No full textThe introduction of a phenyl group on C(2) of 8-azaadenosine increases binding to the adenosine deaminase enzyme (ADA). This stability increment has been quantitatively evaluated in both 8-azaadenosines and 9-(2',3'-dihYdroxypropyl)-8-azaadenines; it resulted nearly equivalent in the two series. 8-Azaadenosine has been synthesized through a new route employing fully protected beta-D-ribofuranosyl-1-azide. Instead, the stability difference in 9-(n-alkyl)-8-azaadenines, owing to the inactivity of the C(2) unsubstituted compounds, could not be evaluated. Consideration of the enantioselectivity of the ADA enzyme toward chiral 9-(2,3'-dihydroxypropyl)-8-azaadenines and 9-(2,3'-dihydroxypropyl)-8-azahypoxanthines allowed the exclusion of an appreciable structural modification in the enzyme-inhibitor complex when hydrogen on C(2) is substituted by an aryl group
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