Lamotte, Yann; Faucher, Nicolas; Sancon, Julien; Pineau, Olivier; Sautet, Stephane; Fouchet, Marie-Helene; Beneton, Veronique; Tousaint, Jean-Jacques; Saintillan, Yannick; Ancellin, Nicolas; Nicodeme, Edwige; Grillot, Didier; Martres, Paul published an article on February 15 ,2014. The article was titled 《Discovery of novel indazole derivatives as dual angiotensin II antagonists and partial PPARγ agonists》, and you may find the article in Bioorganic & Medicinal Chemistry Letters.Name: Methyl 4′-formyl-[1,1′-biphenyl]-2-carboxylate The information in the text is summarized as follows:
Identification of indazole derivatives acting as dual angiotensin II type 1 (AT1) receptor antagonists and partial peroxisome proliferator-activated receptor-γ (PPARγ) agonists is described. Starting from telmisartan, the authors previously described that indole derivatives were very potent partial PPARγ agonists with loss of AT1 receptor antagonist activity. Design, synthesis and evaluation of new central scaffolds led us to the discovery of pyrrazolopyridine then indazole derivatives provided novel series possessing the desired dual activity. Among the new compounds, I was identified as a potent AT1 receptor antagonist (IC50 = 0.006 μM) and partial PPARγ agonist (EC50 = 0.25 μM, 40% max) with good oral bioavailability in rat. The dual pharmacol. of compound I was demonstrated in two preclin. models of hypertension (SHR) and insulin resistance (Zucker fa/fa rat).Methyl 4′-formyl-[1,1′-biphenyl]-2-carboxylate(cas: 144291-47-4Name: Methyl 4′-formyl-[1,1′-biphenyl]-2-carboxylate) was used in this study.
Methyl 4′-formyl-[1,1′-biphenyl]-2-carboxylate(cas: 144291-47-4) belongs to esters. Esters are more polar than ethers but less polar than alcohols. They participate in hydrogen bonds as hydrogen-bond acceptors, but cannot act as hydrogen-bond donors, unlike their parent alcohols. Name: Methyl 4′-formyl-[1,1′-biphenyl]-2-carboxylate
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