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Short Paper | Regular issue | Vol 98, No. 12, 2019, pp.1769-1776
Published online, 26th December, 2019
DOI: 10.3987/COM-19-14193
Studies toward Identifying the Pharmacophore of L-755,807 for Amyloid-β Aggregation Inhibitory Activity

Kenichi Kobayashi,* Kosaku Tanaka III, Yusuke Honma, Momoko Suzuki, and Hiroshi Kogen*

*Graduate School of Pharmaceutical Sciences, Meiji Pharmaceutical University, 2-522-1 Noshio, Kiyose, Tokyo 204-8588, Japan

Abstract

To investigate the structure–activity relationship of L-755,807 for amyloid-β aggregation inhibitory activity, L-755,807 analogs were synthesized and biologically evaluated. The results suggest that a hydrophobic conjugated carbon chain with a terminal hydrophilic functional group is essential for the potent activity. These findings provide a starting point for identifying the pharmacophore of L-755,807.