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Title: Study of the Chemoselectivity of Multicomponent Heterocyclizations Involving 3-Amino-1,2,4-triazole and Pyruvic Acids as Key Reagents, and Biological Activity of the Reaction Products.
Authors: Murlykina, Maryna V.; Sakhno, Yana I.; Desenko, Sergey M.; Shishkina, Svetlana V.; Shishkin, Oleg V.; Sysoiev, Dmytro O.; Kornet, Maryna N.; Schols, Dominique; Goeman, Jan L.; Van der Eycken, Johan; Van der Eycken, Erik V.; Chebanov, Valentin A.
Abstract: Three-component reactions involving 3-amino-1,2,4-triazole, aldehydes, including salicylic aldehydes, and pyruvic acids were studied in detail. The reaction pathway and products of the heterocyclizations could be changed by variation of the reaction parameters. The broad antimicrobial activity of the products was also studied. Compound 9d showed specific anti-influenza virus (A/H1N1) activity, with an IC50 of 0.57 μ M and a CC50 of >100 μ M.
Subjects: CHEMOSELECTIVITY; MICROWAVE chemistry; RING formation (Chemistry); ANTIVIRAL agents; ALDEHYDES
Publication: European Journal of Organic Chemistry, 2015, Vol 2015, Issue 20, p4481
ISSN: 1434-193X
Publication type: Academic Journal
DOI: 10.1002/ejoc.201500469

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Study of the Chemoselectivity of Multicomponent Heterocyclizations Involving 3-Amino-1,2,4-triazole and Pyruvic Acids as Key Reagents, and Biological Activity of the Reaction Products.