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Issue 12, 2012
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A matched molecular pair analysis of in vitro human microsomal metabolic stability measurements for methylene substitution or replacements – identification of those transforms more likely to have beneficial effects

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Abstract

A matched molecular pair analysis (MMPA) was used to study the classic medicinal chemistry transformations of a methylene (–CH2–) into metabolic blocking groups. 1826 matched pairs were identified for 24 transforms and in vitro human microsomal stability analysed. Of these, 4 transforms have shown significant beneficial increase in stability, suggesting these transforms as preferred changes during compound optimisation.

Graphical abstract: A matched molecular pair analysis of in vitro human microsomal metabolic stability measurements for methylene substitution or replacements – identification of those transforms more likely to have beneficial effects

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Publication details

The article was received on 01 Aug 2012, accepted on 19 Sep 2012 and first published on 24 Sep 2012


Article type: Concise Article
DOI: 10.1039/C2MD20226C
Citation: Med. Chem. Commun., 2012,3, 1518-1525
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    A matched molecular pair analysis of in vitro human microsomal metabolic stability measurements for methylene substitution or replacements – identification of those transforms more likely to have beneficial effects

    A. G. Dossetter, Med. Chem. Commun., 2012, 3, 1518
    DOI: 10.1039/C2MD20226C

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