As a part of a research project pertaining to the synthesis of novel candidates as nonsedating, nonclassic H1
histaminergic (H1) blockers with low toxicity profiles, some new 5-substituted aminomethylenepyrimidine-2,4,6-triones
were designed based on the H1 histaminic receptor pharmacophore model. The interactions between the designed
compounds and the H1 receptor were studied using molecular docking on the homology model of H1 receptor. The
designed compounds were synthesized and biologically evaluated for H1-blocking activity; using isolated segments of
guinea pig ileum. Compounds 15,18,19 and 21 exhibited comparable activities to acrivastine (22) as reference nonsedating
drug. The C log P of designed compounds revealed lower values in reference to acrivastine (22) which might indicate
decreased tendency for crossing the blood brain barrier.
Keywords: Synthesis, aminomethylenepyrimidine-2, 4, 6-triones, antihistaminic, pharmacophore modeling, docking.
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