59149-19-8Relevant academic research and scientific papers
Discovery and optimization of arylsulfonyl 3-(pyridin-2-yloxy)anilines as novel GPR119 agonists
Zhang, Jian,Li, An-Rong,Yu, Ming,Wang, Yingcai,Zhu, Jiang,Kayser, Frank,Medina, Julio C.,Siegler, Karen,Conn, Marion,Shan, Bei,Grillo, Mark P.,Eksterowicz, John,Coward, Peter,Liu, Jiwen
, p. 3609 - 3613 (2013/07/25)
We describe the discovery of a series of arylsulfonyl 3-(pyridin-2-yloxy) anilines as GPR119 agonists derived from compound 1. Replacement of the three methyl groups in 1 with metabolically stable moieties led to the identification of compound 34, a potent and efficacious GPR119 agonist with improved pharmacokinetic (PK) properties.
Three new derivatives of 3-amino-1,2-propanediol; their spectral properties and biological evaluation
Morzycki,Maj,Nikitiuk,Kwolek,Malinowska
, p. 249 - 256 (2007/10/03)
Three new derivatives of 3-amino-1,2-propanediol have been synthesized. Full assignments of signals in their 1H- and 13C-NMR spectra are given. The influence of these compounds on the cardiovascular system in the anaesthetized rat was examined. In contrast to CGP 12177 which induced a strong increase in heart rate and a slight increase in blood pressure, compounds 1, 2 and 3 × HCI at doses up to 1 μmol/kg and compound 3 at doses of 0.01 and 0.1 μmol/kg did not change the cardiovascular parameters. The highest dose of compound 3 - 1 μmol/kg caused a very short-lasting decrease in heart rate (by 14%) and in blood pressure (by 25%).
