SYNTHESIS AND PRELIMINARY STRUCTURE-ACTIVITY-RELATIONSHIPS OF 3-FLUORO-4-PYRIDINYL)AMINO]-3-METHYL-1H-INDOL-5-YL METHYL CARBAMATE (P10358),A NOVEL ACETYLCHOLINESTERASE INHIBITOR

Authors
MARTIN LL DAVIS L KLEIN JT NEMOTO P OLSEN GE BORES GM CAMACHO F PETKO WW RUSH DK SELK D SMITH CP VARGAS HM WINSLOW JT EFFLAND RC FINK DM
Citation
Ll. Martin et al., SYNTHESIS AND PRELIMINARY STRUCTURE-ACTIVITY-RELATIONSHIPS OF 3-FLUORO-4-PYRIDINYL)AMINO]-3-METHYL-1H-INDOL-5-YL METHYL CARBAMATE (P10358),A NOVEL ACETYLCHOLINESTERASE INHIBITOR, Bioorganic & medicinal chemistry letters, 7(2), 1997, pp. 157-162
Citations number
22
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
2
Year of publication
1997
Pages
157 - 162
Database
ISI
SICI code
0960-894X(1997)7:2<157:SAPSO3>2.0.ZU;2-V
Abstract
A series of carbamate analogs of besipirdine (HP 749) was synthesized as potential agents with enhanced cholinomimetic properties for the tr eatment of Alzheimer's disease. Compound 5a (P10358, 3-fluoro-4-pyridi nyl)amino]-3-methyl-1H-indol-5-yl methyl carbamate) emerged as a poten t, reversible acetylcholinesterase inhibitor that significantly enhanc ed performance on oral or parenteral administration in earning and mem ory paradigms. (C) 1997, Elsevier Science Ltd.