Drug discovery: phosphinolactone, in vivo bioisostere of the lactol group

作者:Volle Jean Noel*; Filippini Damien; Krawczy Bartlomiej; Kaloyanov Nikolay; Van der Lee Arie; Maurice Tangui; Pirat Jean Luc; Virieux David
来源:Organic and Biomolecular Chemistry, 2010, 8(6): 1438-1444.
DOI:10.1039/b919345f

摘要

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.

  • 出版日期2010-3-21