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Issue 6, 2010
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Drug discovery: phosphinolactone, in vivo bioisostere of the lactol group

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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

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Publication details

The article was received on 17 Sep 2009, accepted on 21 Dec 2009 and first published on 22 Jan 2010


Article type: Paper
DOI: 10.1039/B919345F
Citation: Org. Biomol. Chem., 2010,8, 1438-1444
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    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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