Historical overview on structure-activity relationships among sweeteners

Abstract

The literature on 100 years of research on the structure-activity relationships among sweeteners is reviewed. It started with information on the tastes of many compounds, which were correlated with functional groups of the molecules. In 1967 Shallenberger and Acree indicated a common AH-B moiety among sweeteners. Kier postulated the concept of the third binding site, capable of dispersion bonding, in 1972. New conceptual parameters α, δ and ω for sweeteners were introduced by van der Heijden in 1985 in order to describe three dimensions of the third binding sites versus the AH-B moieties more precisely. In 1990 Tinti and Nofre developed a more extensive model about structure-activity of sweetness assuming the possible presence of eight recognition sites. Application of this model can explain the potency of hyperpotent sweeteners.