This review highlights the role of oxetanes in drug design, improving synthetic accessibility and optimization of physicochemical properties.
The regulatory approval of rilzabrutinib and likely approval of ziresovir provide confidence in using oxetanes as important elements in drug design. While oxetanes have so far been incorporated primarily as pendant groups to optimize physicochemical properties, their use as scaffolding and binding elements presents an exciting opportunity. Enhanced synthetic accessibility to oxetane derivatives will expedite their inclusion in drug discovery campaigns.
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Ishikura et al. (2025) studied this question.
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