Saturated bioisosteres of ortho-disubstituted benzenes (bicyclo[2.1.1]hexanes) were synthesized, characterized and validated. These cores were incorporated into the bioactive compounds Valsartan, Boskalid and Fluxapyroxad instead of the benzene ring. The saturated analogues showed as imilar level of antifungal activity compared to that of Boskalid and Fluxapyroxad.
Saturated bioisosteres of ortho-disubstituted benzenes (bicyclo[2.1.1]hexanes) were synthesized, characterized and validated. These cores were incorporated into the bioactive compounds Valsartan, Boskalid and Fluxapyroxad instead of the benzene ring. The saturated analogues showed as imilar level of antifungal activity compared to that of Boskalid and Fluxapyroxad.
The well-known aminoazoles, 3-amino-5-methylisoxazole and 5-amino-N-aryl-1H-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.
Reactions of 4,7-Dihydro-1,2,4-triazolo [1,5-a]pyrimidines with α,β-Unsaturated Carbonyl Compounds Victoria V. Lipson[a], Irina V. Ignatenko[a], Sergey M. Desenko[b], Svetlana V. Shishkina[b], OlegThe reaction of 5,7-diphenyl-4,7-dihydro-1,2,4-triazolo[1,5-a]pyrimidine (1) with α,β-unsaturated carbonyl compounds 2a-f led to the formation of the alkylated heterocycles 3a-f (Figure 1). However, the reaction of 5-methyl-7-phenyl-4,7-dihydro-1,2,4-triazolo[1,5-a]pyrimidine (5) with 2a-c yielded under the same conditions the triazolo[5,1-b]quinazolines 6a-c (Figure 3). In this case, the alkylation is followed by a cyclocondensation. The structure elucidation of the products is based on ir, ms, 1 H and 13 C nmr measurements and on an X-ray diffraction study.
An X‐ray diffraction study of the title compound, C12H11NO4, has shown that this compound exists in the crystal as the 2‐oxo‐4‐hydroxy tautomer. The formation of two O—H⋯O=C‐type intramolecular hydrogen bonds leads to the elongation of both exocyclic and carboxylic C=O double bonds involved in the hydrogen bonding, causes shortening of the exocyclic C—O single bond, and also affects the C—C bond lengths in the dihydropyridine ring.
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