147404-69-1Relevant articles and documents
Pd black in water as an efficient catalyst of the Suzuki reaction
Kuznetsov,Korolev,Bumag
, p. 1882 - 1883 (2003)
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1,5-disubstituted tetrazole compounds, and preparation method and application thereof
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, (2018/03/24)
The invention discloses 1,5-disubstituted tetrazole compounds, and a preparation method and an application thereof. The 1,5-disubstituted tetrazole compounds have good antitumor activity. The invention also provides a use of the 1,5-disubstituted tetrazol
New telmisartan-derived PPARγ agonists: Impact of the 3D-binding mode on the pharmacological profile
Obermoser, Victoria,Urban, Margarethe E.,Murgueitio, Manuela S.,Wolber, Gerhard,Kintscher, Ulrich,Gust, Ronald
supporting information, p. 138 - 152 (2016/08/30)
In previous studies, the 4′-((2-propyl-1H-benzo[d]imidazol-1-yl)methyl)-[1,1′-biphenyl]-2-carboxylic acid was identified as pharmacophoric core for PPARγ activation. In this structure-activity relationship study the C2-alkyl chain was elongated and the 2-COOH group was changed to a carbamide/carbonitrile or shifted to the 3- or 4-position. Furthermore, the benzo[d]imidazole was exchanged by 2,3-dihydrobenzo[d]thiazole or 1H-indole. C2-propyl derivatives showed the profile of partial agonists, while elongation of the C2-chain to that of an n-heptyl group or a 4-COOH shift changed the pharmacological profile to that of a potent full agonist. This finding can be explained by binding to the LBD in different ligand conformations. Two anchoring points (Tyr473 and Arg288) exist in the LBD, which have to be contacted to achieve receptor activation. In a crystal violet chemosensitivity assay using COS-7?cells and LNCaP cells expressing PPARγ only the carbamide derivatives influenced the cell growth, independently on the presence of the PPARγ. Therefore, receptor mediated cytotoxicity can be excluded.
