68282-49-5Relevant articles and documents
Synthesis and evaluation of new designed multiple ligands directed towards both peroxisome proliferator-activated receptor-γ and angiotensin II type 1 receptor
Meyer, Maxime,Foulquier, Sébastien,Dupuis, Fran?ois,Flament, Stéphane,Grimaud, Linda,Henrion, Daniel,Lartaud, Isabelle,Monard, Gérald,Grillier-Vuissoz, Isabelle,Boisbrun, Michel
supporting information, p. 334 - 352 (2018/09/22)
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.
Preparation of 2-Substituted 4-Chloro-5-Formylimidazole and 5-Formylimidazole
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Page/Page column 4-5, (2008/12/08)
The invention relates to a preparation process for 2-substituted 5-formylimidazoles, wherein the intermediate high-pressurized synthesis of an 2-substituted 4-hydroxymethylimidazole as known in the art is conveniently avoided, and wherein much higher yields are obtained. Instead, it is proposed to prepare such 2-substituted 5-formylimidazoles via a one-pot synthesis involving 2-substituted 4-chloro-5-formylimidazole, thereby employing an additional hydrodehalogenation step. Moreover, it is found that the yield and purity of 2-substituted 4-chloro-5-formylimidazole itself can be significantly improved using a triflate catalyst in the preparation process.
Process for the preparation of formylimidazoles
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, (2008/06/13)
A process for the preparation of formylimidazoles of the general formula: or its tautomers, in which R1 is hydrogen or alkyl, and R2 is hydrogen, halogen or alkyl. In a first stage, an imidazole derivative of the general formula: or its tautomers, in which R1 and R2 are as defined above, is converted, by introducing an amino protective group, into an imidazole derivative of the general formula: or its tautomers, in which R3 is an amino protective group. Such derivative is formylated in a second stage in the presence of an organometallic compound and a suitable electrophile to give an imidazole derivative of the general formula: or its tautomers, in which R1, R2 and R3 are as defined above. Then, in a third stage, the end product of the formula I is obtained by cleaving off the amino protective group.