Ontology highlight
ABSTRACT:
SUBMITTER: Larraufie MH
PROVIDER: S-EPMC4653046 | biostudies-literature | 2015 Nov
REPOSITORIES: biostudies-literature
Bioorganic & medicinal chemistry letters 20150714 21
Introducing a reactive carbonyl to a scaffold that does not otherwise have an electrophilic functionality to create a reversible covalent inhibitor is a potentially useful strategy for enhancing compound potency. However, aldehydes are metabolically unstable, which precludes the use of this strategy for compounds to be tested in animal models or in human clinical studies. To overcome this limitation, we designed ketone-based functionalities capable of forming reversible covalent adducts, while d ...[more]