The Reactivity of α‐Fluorinated Mono‐ and Diketones Uncovers their Potential as Electrophilic Warheads for Reversible Covalent Drugs
Year: 2025
Type: article
Abstract: Fluorinated diketones (FDKs) are electrophilic moieties holding unique molecular properties that make them potential reversible and multifaceted covalent warheads for drug design. To further explore this potential, the multicomponent equilibrium systems of various fluorinated monoketones (FMKs) and FDKs in the presence of the relevant nucleophilic amino acids serine, cysteine, and lysine are studied. These equilibrium systems are investigated using 19 F‐ and 13C‐ NMR spectroscopy, and reveal that for both cysteine and lysine most of the FMKs and FDKs studied may potentially serve as electrophilic warheads for reversible covalent drugs.
Institution: Israel Institute for Biological Research
Language: English
Subfield: Pharmaceutical Science
Domain: Life Sciences
Open Access status: hybrid
Estimated APC paid: $4,330
OpenAlex ID: W4413130737