In 2020, a group of researchers from University of Michigan published a Viewpoint that describes an approaches to mitigate aniline-related toxicities of drugs and drug candidates with the help of saturated isosteres of aniline.
The authors showed that the great part of drugs with idiosyncratic adverse drug reactions (IADRs) were caused by aniline bioactivation and reactive metabolite (RM) formation. The authors copmared physical parameters of some isosters (aminobicyclo[1.1.1]pentane (aminoBCP), aminobicyclo[2.2.2]octane (aminoBCO), aminocubane (aminoCUB) and aminonorbornane (aminoNB)) against the same of aniline and showed that they provided similar three-dimensional characteristics of the parent structure .
We at Chemspace have selected sets with derivatives of these four bioisosters of aniline.
To browse the sets, please use the following links:
The aminoBCP derivatives - 1947 compounds
The aminoBCO derivatives - 1849 compounds
The aminocuban derivatives - 127 compounds
The aminonorbornane derivatives - 1980 compounds
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