Journal
ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 8, Issue 6, Pages 1438-1444Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/b919345f
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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.
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