RIS ID
59474
Abstract
Thirty two new stemofoline analogues were prepared from didehydrostemofoline for studies as AChE inhibitors. C-3 side-chain modified amino, carbamate, triazole and oxazole stemofoline derivatives were prepared. In general the amine derivatives were found to be stronger inhibitors of AChE than their alcohol analogues that we previously reported. Compounds 5 and 26, with small C-3 side chain substituents, were two of the most active inhibitors. Preliminary molecular docking studies suggested that these compounds may inhibit AChE by binding horizontally along the passage of the active-site gorge and block access to acetylcholine.
Grant Number
ARC/DP0879491
Additional Grant Number
Included in
Life Sciences Commons, Physical Sciences and Mathematics Commons, Social and Behavioral Sciences Commons
Publication Details
Sastraruji, K., Sastraruji, T., Ung, A. T., Griffith, R., Jatisatienr, A. & Pyne, S. G. (2012). Synthesis of stemofoline analogues as acetylcholinesterase inhibitors. Tetrahedron, 68 (35), 7103-7115.