• Mariam Al-jomaily Msc in pharmaceutics
  • Tawfeeq Arafat Msc in medicinal chemistry
  • Elham Al-kaissi Msc in medicinal chemistry
  • Mohammad A. Ghattas Msc in medicinal chemistry
  • Zuhair Muhi-eldeen Pro. Medicinal chemistry


Amino acetylenic benzophenone derivative, CNS diseases, H3-antagonist activity, Molecular docking


Objective: To synthesize new amino acetylenic benzophenone derivatives with significant H3-antagonist's activity.

Methods: Amino acetylenic benzophenone derivatives were synthesized from the reaction of 2-hydroxybenzophenone with 3-bromoprop-1-in to generate 2-(prop-2-yn-1-yloxy)-1,3-benzophenone (AZ-1). A mixture of 2-(prop-2-yn-1-yloxy)-1,3-benzophenone, paraformaldehyde, cyclic amine, cuprous chloride (catalytic amount) in peroxide free dioane through Mannich reaction yielded the designed amino acetylenic benzophenone derivatives (AZ-2-7).

Results: The IR, H1-NMR, 13C NMR, and elemental analysis were consistent with the assigned structures. The designers of these compounds as H3-antagonists were based on the nationalization of the important criteria that provide effective inhibitory binding with H3-receptor. Molecular docking results of compounds (AZ-2-7) showed a good H3-receptor antagonistic activity relative to thioperamide of-6 (kcal/mol) especially AZ-2 which has-8.6 (kcal/mol).

Conclusion: Docking results provide a good lead to designing more effective H3 antagonists in managing many CNS diseases like Alzheimer, epilepsy, depression, schizophrenia and many others.


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Author Biography

Mariam Al-jomaily, Msc in pharmaceutics

Dept. of medicinal chemistry


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How to Cite

Al-jomaily, M., T. Arafat, E. Al-kaissi, M. A. Ghattas, and Z. Muhi-eldeen. “SYNTHESIS OF AMINO ACETYLENIC BENZOPHENONE DERIVATIVES AS H3-ANTAGONISTS”. International Journal of Pharmacy and Pharmaceutical Sciences, vol. 7, no. 6, June 2015, pp. 174-9,



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