M-ALKYL ALPHA,ALPHA,ALPHA-TRIFLUOROACETOPHENONES - A NEW CLASS OF POTENT TRANSITION-STATE ANALOG INHIBITORS OF ACETYLCHOLINESTERASE

Authors
NAIR HK QUINN DM
Citation
Hk. Nair et Dm. Quinn, M-ALKYL ALPHA,ALPHA,ALPHA-TRIFLUOROACETOPHENONES - A NEW CLASS OF POTENT TRANSITION-STATE ANALOG INHIBITORS OF ACETYLCHOLINESTERASE, Bioorganic & medicinal chemistry letters, 3(12), 1993, pp. 2619-2622
Citations number
16
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
3
Issue
12
Year of publication
1993
Pages
2619 - 2622
Database
ISI
SICI code
0960-894X(1993)3:12<2619:MA-ANC>2.0.ZU;2-H
Abstract
A series of m-alkyl alpha,alpha,alpha-trifluoroacetophenones (1-5) was synthesized and evaluated as inhibitors of acetylcholinesterase from Torpedo californica. All ketones (1-5) were found to be potent inhibit ors of the enzyme; m-t-butyl alpha,alpha,alpha-trifluoroacetophenone ( 4) was the most potent inhibitor with a K(i) value of 3.7 pM.