Abstract
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.
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