210962-92-8Relevant academic research and scientific papers
Preparation method of entresto key intermediate
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, (2018/03/01)
The invention relates to the technical field of medicines and particularly relates to a preparation method of a novel entresto key intermediate. When the method provided by the invention is used for preparing the entresto key intermediate, the method is mild in reaction conditions and is green and environmentally friendly; meanwhile, the yield of the method is higher than that of the existing preparation method; the method is economical and effective and is suitable for large-scale industrial production.
FURANE DERIVATIVES AS INHIBITORS OF ATAD2
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Page/Page column 116; 117; 118; 119, (2017/07/19)
The invention relates to fur an e derivatives of formula (I) as inhibitors of ATAD2, a process for their preparation and use thereof.
Development of the first potential covalent inhibitors of anandamide cellular uptake
Moriello, Aniello Schiano,Balas, Laurence,Ligresti, Alessia,Cascio, Maria Grazia,Durand, Thierry,Morera, Enrico,Ortar, Giorgio,Di Marzo, Vincenzo
, p. 2320 - 2332 (2007/10/03)
On the basis of the chemical structures of two previously developed metabolically stable and relatively potent inhibitors of anandamide uptake, OMDM-1,2, two series of potential covalent inhibitors of anandamide cellular reuptake, which might be used for the molecular characterization of the protein(s) involved in the membrane transport of endocannabinoids, have been designed and synthesized. Most of the compounds inhibited uptake to a varied extent and in a generally enantio-sensitive manner when co-incubated with [ 14C]anandamide, but only three of them, the photoactivatable 1a (OMDM-37), 1b (OMDM-39), and 8 (Lo395), also produced a significant inhibition of uptake following the preincubation only of the cells, and this effect was significantly enhanced following UV exposure only in the case of 8. None of the new compounds inhibited [14C]anandamide hydrolysis with IC 50 50 μM, except for 1b.
