114772-38-2Relevant articles and documents
Synthesis method of 4-bromomethyl-2-methyl formate biphenyl
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Paragraph 0025; 0031-0032; 0038, (2021/07/14)
The invention discloses a synthesis method of 4-bromomethyl-2-methyl formate biphenyl. The method comprises the following steps: performing bromination reaction in a mode of synchronously dropwise adding bromine and hydrogen peroxide, re-oxidizing hydrobromic acid formed after the reaction into bromine, and performing bromination reaction again, so that the bromine can fully participate in the reaction so as to reduce the use amount of bromine raw materials and improve the yield of the 4-bromomethyl-2-methyl formate biphenyl, waste difficult to treat cannot be generated, hydrogen peroxide is cheap and easy to obtain, and the production cost is remarkably saved.
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.
Synthesis of new biphenyl-substituted quinoline derivatives, preliminary screening and docking studies
Shashikumar, Nellisara D,Krishnamurthy, Ganganaika,BhojyaNaik, Halehatti S,Lokesh, Mayasandra R,Jithendrakumara, Kaginalli S
, p. 205 - 212 (2016/03/01)
New quinoline derivatives containing biphenyl ring were synthesized and characterized by IR, 1H NMR and mass spectral studies. The synthesized compounds were screened for antimicrobial, anthelmintic activities as well as free radical scavenging property against the DPPH radical. The minimum inhibition concentration values showed promising inhibiting activity and are potent biological agents. The compounds showed minimum binding energy towards β-tubulin. The compounds 11a, 11c, 13c and 13d have good affinity towards the active pocket and may be considered as a good inhibitor of β-tubulin.
