QUANTITATIVE STRUCTURE-ACTIVITY-RELATIONSHIPS IN A SET OF THIAZOLIDIN-4-ONES ACTING AS H-1-HISTAMINE ANTAGONISTS

A series of 2-(3- and 4-substituted -(N,N-dimethylamino)propyl]-1,3-th iazolidin-4-ones acting as H-1-antihistaminics was investigated with a combined Hansch-CoMFA approach. The substituents at the 3- and 4-posi tions of the phenyl ring have been described through steric, electroni c and hydrophobic parameters and correlated with pA(2) values. The obt ained quantitative models suggest that affinity to the receptor is pro moted by hydrophobic and small 4-substituents and by 3- and 4-substitu ents generating a positive electrostatic potential towards a complemen tary receptor region.