282527-62-2Relevant academic research and scientific papers
Lipase-catalysed synthesis of new acetylcholinesterase inhibitors: N- benzylpiperidine aminoacid derivatives
Martinez, Ana,Lanot, Cristina,Perez, Concepcion,Castro, Ana,Lopez-Serrano, Paloma,Conde, Santiago
, p. 731 - 738 (2000)
New acetylcholinesterase inhibitors were synthetized via a lipase- mediated regioselective amidation using Candida antarctica lipase B as a biocatalyst in the key step. The new compounds have two different structural fragments: a N-benzylpiperidine moiety to anchor the enzyme active site and a dicarboxylic aminoacid to act as a biological carrier. Some analogues of N- benzylpiperazine were also synthesised and studied but they did not display AChE inhibitor activity. A preliminary structure-activity relationship study was performed employing some computational techniques as similarity indices and electrostatic potential maps. (C) 2000 Published by Elsevier Science Ltd.
