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Boosting Anti-Inflammatory Potency of Zafirlukast by Designed Polypharmacology

: Schierle, S.; Flauaus, C.; Heitel, P.; Willems, S.; Schmidt, J.; Kaiser, A.; Weizel, L.; Goebel, T.; Kahnt, A.S.; Geisslinger, G.; Steinhilber, D.; Wurglics, M.; Rovati, G.E.; Schmidtko, A.; Proschak, E.; Merk, D.


Journal of medicinal chemistry 61 (2018), No.13, pp.5758-5764
ISSN: 0022-2623
ISSN: 1520-4804
Journal Article
Fraunhofer IME ()

Multitarget design offers access to bioactive small molecules with potentially superior efficacy and safety. Particularly multifactorial chronic inflammatory diseases demand multiple pharmacological interventions for stable treatment. By minor structural changes, we have developed a close analogue of the cysteinyl-leukotriene receptor antagonist zafirlukast that simultaneously inhibits soluble epoxide hydrolase and activates peroxisome proliferator-activated receptor γ. The triple modulator exhibits robust anti-inflammatory activity in vivo and highlights the therapeutic potential of designed multitarget agents.