European Journal of Medicinal Chemistry p. 334 - 352 (2018)
Update date:2022-08-30
Topics:
Meyer, Maxime
Foulquier, Sébastien
Dupuis, Fran?ois
Flament, Stéphane
Grimaud, Linda
Henrion, Daniel
Lartaud, Isabelle
Monard, Gérald
Grillier-Vuissoz, Isabelle
Boisbrun, Michel
Because of the complex biological networks, many pathologic disorders fail to be treated with a molecule directed towards a single target. Thus, combination therapies are often necessary, but they have many drawbacks. An alternative consists in building molecules intended to interact with multiple targets, called designed multiple ligands. We followed such a strategy in order to treat metabolic syndrome, by setting up molecules directed towards both type 1 angiotensin II (AT1) receptor and peroxisome proliferator-activated receptor-γ (PPAR-γ). For this purpose, many molecules were prepared by merging both pharmacophores following three different strategies. Their ability to activate PPAR-γ and to block AT1 receptors were evaluated in vitro. This strategy led to the preparation of many new PPAR-γ activating and AT1 blocking molecules. Among them, some exhibited both activities, highlighting the convenience of this approach.
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