Design, Synthesis, and Inhibitory Activity of Potent, Photoswitchable Mast Cell Activation Inhibitors

Willem A. Velema, Marco van der Toorn, Wiktor Szymanski*, Ben L. Feringa

*Bijbehorende auteur voor dit werk

OnderzoeksoutputAcademicpeer review

34 Citaten (Scopus)
520 Downloads (Pure)

Samenvatting

Allergic reactions affect millions of people worldwide. The need for new and effective antiallergic agents is evident, and insight into the underlying mechanisms that lead to allergic events is necessary. Herein, we report the design, synthesis, and activity of photoswitchable mast cell activation inhibitors. In mast cell degranulation assays, these inhibitors possess significantly greater potency than an original, chromone-based antiallergic agent. Furthermore, one of the photoswitchable inhibitors shows a significant difference in inhibitory activity between its two photoisomeric forms. Further optimization could ultimately lead to a photoswitchable compound suitable for studying mechanisms involved in allergic reactions in a novel manner, with activity addressable by light and with precise spatiotemporal control over events at the molecular level.

Originele taal-2English
Pagina's (van-tot)4456-4464
Aantal pagina's9
TijdschriftJournal of Medicinal Chemistry
Volume56
Nummer van het tijdschrift11
DOI's
StatusPublished - 13-jun-2013

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