Recent Advances and Outlook for the Isosteric Replacement of Anilines

Many promising drug candidates and pharmaceutical compounds fail due to idiosyncratic adverse drug reactions (IADRs), often arising from the formation of reactive metabolites. Among the “structural alerts” responsible, anilines are well-known to undergo deleterious metabolic processing, yet isosteri...

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Bibliographic Details
Published in:ACS medicinal chemistry letters 2020-10, Vol.11 (10), p.1785-1788
Main Authors: Sodano, Taylor M, Combee, Logan A, Stephenson, Corey R. J
Format: Article
Language:English
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Summary:Many promising drug candidates and pharmaceutical compounds fail due to idiosyncratic adverse drug reactions (IADRs), often arising from the formation of reactive metabolites. Among the “structural alerts” responsible, anilines are well-known to undergo deleterious metabolic processing, yet isosteric replacement strategies remain limited. Herein we discuss current art and potential new avenues of saturated isosteres to mitigate aniline-related toxicities.
ISSN:1948-5875
1948-5875
DOI:10.1021/acsmedchemlett.9b00687