ChemInform Abstract: Design, Synthesis, and Molecular‐Modeling Study of Aminothienopyridine Analogues of Tacrine for Alzheimer′s Disease.

Abstract

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.