Bioactivation of Structural Alerts

With the biochemistry magic available to the liver, it’s a wonder that anything we consume is well-tolerated. Even carboxylic acids are structural alerts as they can be converted to bioreactive acyl glucoronides. The best we can do as drug hunters is minimize the risk of toxic metabolite formation and apply assays appropriately to select compounds most suited to the disease being treated. Here’s a list of the most commonly encountered bioactivatable functional groups and their corresponding reactive metabolites.

Bioactivation of structural alerts cheat sheet

and this recent article by Alf Claesson and Alexander Minidis:

“Systematic Approach to Organizing Structural Alerts for Reactive Metabolite Formation from Potential Drugs.” Chem. Res. Toxicol. 2018, 31, 389-411.

Hope this helps. Happy hunting! Explore drughunter.com for more.

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