477775-44-3Relevant academic research and scientific papers
Aryl and Heteroaryl N1-Tetrazoles through Ligand-Free Suzuki-Reaction under Aerobic, Aqueous Conditions
Seifried, Marco,Knoll, Christian,Giester, Gerald,Welch, Jan M.,Müller, Danny,Weinberger, Peter
, p. 2416 - 2424 (2017)
Substituted 1-biaryl-1H-tetrazoles are classically obtained from the corresponding 1-aminobiaryls, limiting the selection of substrates. The development and substrate scope of a green, ligand-free Suzuki protocol in aqueous media under ambient atmosphere, leading to 1-biaryl- and heteroaryl-substituted 1H-tetrazoles in very good to excellent yields is presented. The combination of PdCl2/NEt3/H2O/EtOH was found to combine high yields and high purity for all substrates investigated. Comparative experiments investigating the reaction rate showed that the tetrazole does not act as a ligand for the palladium catalyst.
Selective angiotensin II AT2 receptor agonists with reduced CYP 450 inhibition
Mahalingam,Wan, Yiqian,Murugaiah,Wallinder, Charlotta,Wu, Xiongyu,Plouffe, Bianca,Botros, Milad,Nyberg, Fred,Hallberg, Anders,Gallo-Payet, Nicole,Alterman, Mathias
experimental part, p. 4570 - 4590 (2010/09/12)
Structural alterations to the benzylic position of the first drug-like selective angiotensin II AT2 receptor agonist (1) have been performed, with the emphasis to reduce the CYP 450 inhibitory property of the initial structure. The imidazole moiety, responsible for the CYP 450 inhibitory effect in 1, was replaced with various heterocycles. In addition, the modes of attachment of the heterocycles, that is, carbon versus nitrogen attachment, and introduction of carbonyl functionalities to the benzylic position have been evaluated. In all the three series, AT2 receptor ligands with affinity in the lower nanomolar range were identified. None of the analogues, regardless of the substituents, exhibited any affinity for the AT1 receptor. Compounds with substantially reduced inhibition of the CYP 450 enzymes were obtained. Among them the compound 60 was found to induce neurite elongation in NG 108-15 cells and served as potent AT2 selective agonist.
INHIBITORS OF VEGF RECEPTOR AND HGF RECEPTOR SIGNALING
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Page/Page column 93, (2010/02/15)
The invention relates to the inhibition of vascular endothelial growth factor (VEGF) receptor signaling and hepatocyte growth factor (HGF) receptor signaling. The invention provides compounds and methods for inhibiting VEGF receptor signaling and HGF receptor signaling. The invention also provides compositions and methods for treating cell proliferative diseases and conditions
