Issue 6, 2010

Drug discovery: phosphinolactone, in vivo bioisostere of the lactolgroup

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.

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

Supplementary files

Article information

Article type
Paper
Submitted
17 Sep 2009
Accepted
21 Dec 2009
First published
22 Jan 2010

Org. Biomol. Chem., 2010,8, 1438-1444

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

J. Volle, D. Filippini, B. Krawczy, N. Kaloyanov, A. Van der Lee, T. Maurice, J. Pirat and D. Virieux, Org. Biomol. Chem., 2010, 8, 1438 DOI: 10.1039/B919345F

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