1.
Org Biomol Chem
; 8(6): 1438-44, 2010 Mar 21.
Article
in English
| MEDLINE
| ID: mdl-20204219
ABSTRACT
In drug discovery, structural modifications over the lead molecule are often crucial for the development of a drug. Herein, we reported the first in vivo bioisosteric effect of phosphinolactone function in relation to the lactol group constituting the bioactive molecule: Hydroxybupropion. The preparation of phosphinolactone analogues and their antidepressant evaluation towards forced swimming test in mice showed that biological activity was regained and even strengthen.