Design, Synthesis and H1 - Antihistaminic Activity of Novel Thieno [2, 3-d] pyrimidinones

Abstract

Some of the fused pyrimidinones were reported from our laboratory with antihistaminic and bronchodilatory activities. As part of our ongoing research programme on the potential utility of thienopyrimidines, a novel series of compounds were designed based on the general pharmacophore model for H1- antihistaminic agents. The designed molecules were synthesized and evaluated for antihistaminic activity and anticholinergic activity. Various descriptors like HOMO (Highest Occupied Molecular Orbital), LUMO (Lowest Unoccupied Molecular Orbital) and clogP that can influence the sedative and anticholinergic activity of the molecules were computed while designing the molecules using Chem Office-2008. All the virtual screening data was correlating with the experimental values.