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The isomeric and tautomeric structure of I and II type monoacylated 5‐amino‐1,2,4‐triazole derivatives was studied with the help of their ir, uv, pmr and cmr spectra as well as model compounds prepared for this purpose. It was stated that the structure of the I type ring‐acylated derivatives is 2o and those of their II type isomers is 5a.

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The correct isomeric and tautomeric structure of different 1‐ and 2‐R1‐3‐R2,R3‐amino‐5‐amino‐1,2,4‐triazole derivatives prepared from the corresponding N‐cyano‐N'‐R2,R3‐S‐methyl‐isothioureas and the corresponding hydrazines was proved with the help of their ir, uv, 1H‐nmr and 13C‐nmr spectra as well as the uv spectra of the Schiff bases of an isomeric pair.

The syntheses and antiviral properties of the new acylated 1,2,4-triazole derivatives 4 are described. In cel1 culture experiments 6 out of 99 compounds specifically inhibit rubelia virus replication to a high degree. Structure-activity relationships are discussed. Neue acylierîe 1,2,4-Tnazoie als antivirale WirkstoffeDie Synthese und die antivirale Aktivität einiger neuer acylierten 1,2,4-Triazoie 4 wird beschrieben. In Zell-Kulturen erwiesen sich 6 von 99 Verbindungen als hoch wirksam und spezifisch gegen das Rubella Virus. Struktur-Aktivitäts-Beziehungen werden diskutiert. Antiviral chemotherapy must be directed to the development of compounds with activity against virus replication without affecting any cellular metabolic processes.The most valuable compounds specifically inhibit virus multiplication; 9-(2-hydroxyethoxymethy1)guanine and (E)-5-(2-bromovinyl)-deoxyuridine have been reported as exhibiting highly selective antiviral activity against the growth of herpes simplex virus14).Til1 the present time there have been only few papers about the triazole derivatives posessing antiviral activity . Thus 3-mercapto-5-(4-pyridyl)-4H-l,2,4-triazole is active oraily against neurovaccinia in mice". Other 1,2,4-triazole derivatives weakly inhibit the multiplication of ranikhet disease virus in a stationary culture of chorioallantoic membranes of chick embryo6). Triazolotriazino[5,6-blindole derivatives show some activity against herpes simplex virus7). 1-P-D-ribofuranosyl-1,2,4-triazole-3-carboxarnide is a nucleoside which inhibits some of the DNA-and RNA-virus rep~ications"~).The present study reports the synthesis of new acylated 1,2,4-triazoles with a selective antiviral activity against the rubella virus infected cell"'). The synthetic procedure followed the route below.The known reaction of N-cyano-carbonimidodithioic acid diaikyl esters 1 with hydrazine offered a good possibility to get large variable starting material~l'-'~), 3-alkylthio-S-amino-lH-l,2,4-triazoles 2 in a simple way.2 can be acylated in an organic aprotic solvent, e. g. dioxane in the presence of an organic base, e. g. pyridine at room temperature, to the I-benzoylated triazoles 3.3 can be submitted to a thermal rearrangement either in an organic inert solvent, e. g. sulfolane, dimethylformamide, dimethylsulfoxide or without solvent at a temperature of