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J Med Chem. 1995 Sep 1;38(18):3645-51.

Synthesis and evaluation of 5-amino-5,6,7,8-tetrahydroquinolinones as potential agents for the treatment of Alzheimer's disease.

Author information

1
Department of Medicinal Chemistry, Hoechst-Roussel Pharmaceuticals, Inc, Somerville, New Jersey 08876, USA.

Abstract

A series of 5-amino-5,6,7,8-tetrahydroquinolinones was designed and synthesized as acetylcholinesterase inhibitors. The compounds are related to hyperzine A, a naturally occurring cholinesterase inhibitor. They inhibit acetylcholinesterase in vitro, and many are active in vivo in reversing a scopolamine-induced impairment of 24 h memory in a passive avoidance paradigm. Although these compounds were designed as partial structures of huperzine A, it is unlikely that they bind to the enzyme in a similar fashion, since they lack the unsaturated three-carbon bridge of huperzine A and both the quinolinone nitrogen and the amino group must be substituted in order to obtain good enzyme affinity.

PMID:
7658452
DOI:
10.1021/jm00018a025
[Indexed for MEDLINE]

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