Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry, Pharmaceutical Sciences and Computational Chemistry

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Abstract

Synthesis and Pharmacological Screening of New Thienopyridines for the treatment of Alzheimer├ó┬?┬?s disease

Author(s): Afaf El-Malah, Zeinab Mahmoud and Mai A. AbdEl Fattah

Alzheimer is a multitargeting brain-hitting disease. The need to prepare and screen new agents is endless. Novel thienopyridine-tacrine analogues 4a,b – 8a,b and 9 have been designed, synthesized and biologically screened against cholinesterase inhibition activity. Two compounds 7a and 7b were found active. Compound 7b exceeded tacrine as a cholinesterase inhibitor. The docking studies explained this activity as compound 7b exhibited similar binding affinity to the acetylcholinesterase enzyme as with tacrine in addition to an extra hydrogen bonding


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