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Design, Synthesis, and Molecular‐modeling Study of Aminothienopyridine Analogues of Tacrine for Alzheimer's Disease
Author(s) -
Badran Mohga M.,
Hakeem Maha Abdel,
AbuelMaaty Suzan M.,
ElMalah Afaf,
Salam Rania M. Abdel
Publication year - 2010
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200900226
Subject(s) - tacrine , chemistry , acetylcholinesterase , cholinesterase , stereochemistry , aché , pharmacology , biochemistry , enzyme , biology
2‐Amino‐3‐cyanothiophenes were successfully condensed with a number of cycloalkanones to afford tacrine analogues in a one‐step reaction mediated with Lewis acid. The newly synthesized compounds have been tested for their ability to inhibit acetylcholine esterase (AChE) activity using tacrine as standard drug. Some of the tested compounds showed moderate inhibitory activity in comparison with tacrine, especially compounds 6a which displayed the highest inhibitory activity. Furthermore, molecular‐modeling studies were performed in order to rationalize the obtained biological results.