22934-47-0Relevant articles and documents
Synthesis and biological evaluation of phenoxyacetic acid derivatives as novel free fatty acid receptor 1 agonists
Wang, Xuekun,Zhao, Tianxiao,Yang, Baowei,Li, Zheng,Cui, Jian,Dai, Yuxuan,Qiu, Qianqian,Qiang, Hao,Huang, Wenlong,Qian, Hai
, p. 132 - 140 (2015/02/18)
Free fatty acid receptor 1 (FFA1) is a new potential drug target for the treatment of type 2 diabetes because of its role in amplifying glucose-stimulated insulin secretion in pancreatic β-cell. In the present studies, we identified phenoxyacetic acid derivative (18b) as a potent FFA1 agonist (EC50 = 62.3 nM) based on the structure of phenylpropanoic acid derivative 4p. Moreover, compound 18b could significantly improve oral glucose tolerance in ICR mice and dose-dependently reduced glucose levels in type 2 diabetic C57BL/6 mice without observation of hypoglycemic side effect. Additionally, compound 18b exhibited acceptable PK profiles. In summary, compound 18b with ideal PK profiles exhibited good activity in vitro and in vivo, and might be a promising drug candidate for the treatment of diabetes mellitus.
Direct B-alkyl Suzuki-Miyaura cross-coupling of trialkyl-boranes with aryl bromides in the presence of unmasked acidic or basic functions and base-labile protections under mild non-aqueous conditions
Wang, Bing,Sun, Hui-Xia,Sun, Zhi-Hua,Lin, Guo-Qiang
experimental part, p. 415 - 422 (2009/10/23)
An efficient and chemoselective palladium-catalyzed direct B-alkyl Suzuki-Miyaura cross-coupling of trialkylboranes with diversely functionalized aryl bromides is described. A wide variety of unmasked acidic or basic functions are tolerated. The mild non-
B-Alkyl Suzuki-Miyaura cross-coupling of tri-n-alkylboranes with arylbromides bearing acidic functions under mild non-aqueous conditions
Sun, Hui-Xia,Sun, Zhi-Hua,Wang, Bing
experimental part, p. 1596 - 1599 (2009/06/18)
An efficient and chemoselective Pd-catalyzed B-alkyl Suzuki-Miyaura cross-coupling of tri-n-alkylboranes with arylbromides possessing acidic functions is described. This protocol features the relatively weak base Cs2CO3 and mild non-
Synthesis and Structure-Activity Relationships among α-Adrenergic Receptor Agonists of the Phenylethanolamine Type
Leclerc, Gerard,Bizec, Jean Claude,Bieth, Nicole,Schwartz, Jean
, p. 738 - 744 (2007/10/02)
Nineteen arylethanolamine derivatives related to norepinephrine were prepared and tested for α-adrenergic stimulant activity.In one series the analogues possess a p-hydroxy function, while the meta position is substituted by methyl, ethyl, isopropyl, cyclohexyl, fluoro, chloro, iodo, carboxy, carbomethoxy, and methylsulfamido groups.The other series is meta hydroxylated with the para position substituted by the same groups.The influence of these groups upon the α-adrenergic activity is discussed, and the compounds are compared to octopamine, normetanephrine,norepinephrine, and norphenylephrine.It has been found that the introduction of an isopropyl, cyclohexyl, and fluoro group in the meta position of octopamine improves its affinity by three, five, and six times, respectively, whereas when these groups are introduced in the para position of norphenylephrine their effects are always detrimental.The most active compound, α-(aminomethyl)-(4-fluoro-3-hydroxyphenyl)methanol (44), has about one-hundreth the affinity and the same intrinsic activity as norepinephrine.
