Diazaborines as New Inhibitors of Human Neutrophil Elastase.

ABSTRACT: Boronic acids (BAs) are a prominent functionality extensively used to design biologically active compounds and functional biomaterials. Boronic acids open shell can lead to unspecific reactivity of BAs with endogenous nucleophiles and to undesired off-target effects. Here, diazaborines are presented as a new class of boron-based warheads for serine proteases inhibition, in which the boron function is stabilized in the form of an aromatic boron-based heterocycle. In this study, diazaborines were readily synthesized in a single step in yields up to 96%, without any chromatographic operation and were shown to reversibly inhibit human neutrophil elastase (HNE) serine protease with IC₅₀ values in the low μM range. Diazaborines were also selective toward HNE, as no inhibition was obse

SUBMITTER: Antonio JPM 

PROVIDER: S-EPMC6068696 | biostudies-literature | 2018 Jul

REPOSITORIES: biostudies-literature