122801-57-4Relevant articles and documents
Synthesis, structural, and electron topographical analyses of a dialkylbiaryl phosphine/arene-ligated palladium(I) dimer: Enhanced reactivity in Suzuki-Miyaura coupling reactions
Barder, Timothy E.
, p. 898 - 904 (2006)
The treatment of bis(2-(dicyclohexylphosphino)-2′,6′- dimethoxybiphenyl)PdCl2 with AgBF4 produces an air-stable phosphine/arene-ligated Pd(I) dimer with two seemingly identical Pd-arene interactions by X-ray crystallography. However, NMR and theoretical electron topographical analyses of this complex distinguish between these two interactions. One interaction is classified as an arenium-like complex, while the other is classified as a π-interaction. Additionally, this complex is a suitable precatalyst for high yielding Suzuki-Miyaura coupling reactions in short reaction times.
Design, synthesis and biological evaluation of novel FFA1/GPR40 agonists: New breakthrough in an old scaffold
Li,Liu, Chunxia,Yang, Jianyong,Zhou,Ye, Zhiwen,Feng,Yue, Na,Tong,Huang, Wenlong,Qian, Hai
, p. 608 - 622 (2019/07/05)
Based on an old phenoxyacetic acid scaffold, CPU014 (compound 14) has been identified as a superior agonist by comprehensive exploration of structure-activity relationship. In vitro toxicity study suggested that CPU014 has lower risk of hepatotoxicity than TAK-875. During acute toxicity study (5–500 mg/kg), a favorable therapeutic window of CPU014 was observed by evaluation of plasma profiles and liver slices. Moreover, CPU014 promotes insulin secretion in a glucose-dependent manner, while no GLP-1 secretion has been enhanced. Other than good pharmacokinetic properties, CPU014 significantly improved glucose tolerance both in normal and diabetic models without the risk of hypoglycemia. These subversive findings provided a safer candidate CPU014, which is currently in preclinical study to assess its potential for the treatment of diabetes.
5-HT7receptor modulators: Amino groups attached to biphenyl scaffold determine functional activity
Kim, Youngjae,Park, Hyeri,Lee, Jeongeun,Tae, Jinsung,Kim, Hak Joong,Min, Sun-Joon,Rhim, Hyewhon,Choo, Hyunah
, p. 180 - 190 (2016/08/02)
5-HT7receptor (5-HT7R) agonists and antagonists have been reported to be used for treatment of neuropathic pain and depression, respectively. In this study, as a novel scaffold for 5-HT7R modulators, we designed and prepared a series of biphenyl-3-yl-methanamine derivatives with various amino groups. Evaluation of functional activities as well as binding affinities of the title compounds identified partial agonists (EC50?=?0.55–3.2?μM) and full antagonists (IC50?=?5.57–23.1?μM) depending on the amino substituents. Molecular docking study suggested that the ligand-based switch in functional activity from agonist to antagonist results from the size of the amino groups and thereby different binding modes to 5-HT7R. In particular, interaction of the ligand with Arg367 of 5-HT7R is shown to differentiate agonists and antagonists. In the pharmacophore model study, two distinct pharmacophore models can tell whether a ligand is an agonist or an antagonist. Taken together, this study provides valuable information for designing novel compounds with selective agonistic or antagonistic properties against 5-HT7R.