Description and references

Physostigmine, q.v., analog; acetylcholinesterase inhibitor that reduces β-amyloid precursor protein (β-APP) formation. Prepn: M. Polonovski, Bull. Soc. Chim. Fr. 19, 46 (1916). See also: M. Pomponi et al., EP 154864; M. Brufani et al., US 5306825 (1985, 1994 both to Consig. Naz. Delle Ricerche). Anticholinesterase activity: M. Brzostowska et al., Med. Chem. Res. 2, 238 (1992). Pharmacology: S. Iijima et al., Psychopharmacology 112, 415 (1993). Pharmacokinetics: N. H. Greig et al., Acta Neurol. Scand. Suppl. 176, 74 (2000). Mode of action study for regulating β -APP expression: K. T. Y. Shaw et al., Proc. Natl. Acad. Sci. USA 98, 7605 (2001). Review of total synthesis and biological activity: N. H. Greig et al., Med. Res. Rev. 15, 3-31 (1995); A. Brossi et al., Aust. J. Chem. 49, 171-181 (1996). Review of development and therapeutic potential: U. Thatte, IDrugs 3,1222-1228 (2000).

Properties

Derivative