Design and synthesis of thienopyridines as novel templates for acetylcholinesterase inhibitors

作者：Badran Mohga M; Hakeem Maha Abdel; Abuel Maaty Suzan M^*; El Malah Afaf; Salam Rania M Abdel

来源：Medicinal Chemistry Research, 2013, 22(9): 4087-4095.

DOI：10.1007/s00044-012-0403-5

• Synthesis
• Thienopyridines
• AChE inhibitors
• Alzheimer%26apos
• s disease

New dual binding site acetylcholinesterase (AChE) inhibitors have been designed and synthesized as a new drug candidate for the treatment of Alzheimer%26apos;s disease (AD) through the binding to both catalytic and peripheral sites of the enzyme. Therefore, a series of thienopyridine analogs of tacrine were synthesized and investigated for their ability to inhibit the activity of AChE in comparison with tacrine. All the compounds were found to inhibit AChE activity, especially compounds 7b and 11a, which were found to be more potent than tacrine.

• 出版日期2013-9