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Article Dans Une Revue Organic & Biomolecular Chemistry Année : 2010

Drug Discovery: Phosphinolactone as Ultimate Bioisostere of the Lactol Group

Résumé

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.

Dates et versions

hal-00461530 , version 1 (04-03-2010)

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Jean-Noël Null Volle, Damien Fillipini, B. Krawczy, N. Kaloyanov, Arie van Der Lee, et al.. Drug Discovery: Phosphinolactone as Ultimate Bioisostere of the Lactol Group. Organic & Biomolecular Chemistry, 2010, 8, pp.1438-1444. ⟨10.1039/b919345f⟩. ⟨hal-00461530⟩
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