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Computer-aided Design, Synthesis, and Biological Evaluation of 5- Substituted Aminomethylenepyrimidine-2,4,6-Triones as H1 Antihistaminic Agents (Part2)

[ Vol. 10 , Issue. 1 ]

Author(s):

Rasha Y. Elbayaa   Pages 66 - 73 ( 8 )

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.

Keywords:

Synthesis, aminomethylenepyrimidine-2, 4, 6-triones, antihistaminic, pharmacophore modeling, docking.

Affiliation:

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Alexandria, 1 Elkhartoum Square, Azarita, Alexandria, Egypt.



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