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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. [ABSTRACT FROM AUTHOR]

Peptidomimetics with a substituted imidazo[1,2- a ]pyridine fragment were synthesized by a tandem of Groebke-Blackburn-Bienaymé and Ugi reactions. The target products contain substituted imidazo[1,2- a ]pyridine and peptidomimetic moieties as pharmacophores with four diversity points introduced from readily available starting materials, including scaffold diversity. A small focused compound library of 20 Ugi products was prepared and screened for antibacterial activity., (Copyright © 2023, Kolomiiets et al.)

The well-known aminoazoles, 3-amino-5-methylisoxazole and 5-amino- N -aryl-1 H -pyrazole-4-carboxamides, were studied as an amine component in Ugi and Groebke-Blackburn-Bienaymé multicomponent reactions. The first example of an application of aminoazoles in an Ugi four-component reaction was discovered and novel features of a Groebke-Blackburn-Bienaymé cyclocondensation are established and discussed. The heterocycles obtained were evaluated for their antibacterial activity and several of them demonstrated a weak antimicrobial effect, but for most of the compounds a 30-50% increase in biomass of Gram-positive strains (mainly B. subtilis ) compared to control was observed.