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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.

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Design, Synthesis, and Molecular-Modeling Study of Aminothienopyridine Analogues of Tacrine for Alzheimer's Disease. -Starting compounds (I) are obtained by classical Gewald reaction. Condensation of (I) with a number of cycloalkanones affords several tacrine analogues in a one-step reaction mediated by Lewis acids. Some of the newly prepared compounds, e.g. (III), (Va), and (Vb), show significant AChE inhibition activity. (IIIb) is the most active derivative with an activity similar to that of tacrine. -(BADRAN, M. M.; HAKEEM*, M. A.; ABUEL-MAATY, S. M.; EL-MALAH, A.; SALAM, R. M. A.; Arch. Pharm. (Weinheim, Ger.) 343 (2010) 10, 590-601, http://dx.