4.5 Editorial Material

Recent Advances and Outlook for the Isosteric Replacement of Anilines

期刊

ACS MEDICINAL CHEMISTRY LETTERS
卷 11, 期 10, 页码 1785-1788

出版社

AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.9b00687

关键词

Bioisosteres; structural alerts; reactive metabolites; anilines; aminonorbornanes

资金

  1. NIH NIGMS [R01-GM127774]

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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.

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