95958-02-4Relevant academic research and scientific papers
Alkene Oxyamination Using Malonoyl Peroxides: Preparation of Pyrrolidines and Isoxazolidines
Alamillo-Ferrer, Carla,Curle, Jonathan M.,Davidson, Stuart C.,Lucas, Simon C. C.,Atkinson, Stephen J.,Campbell, Matthew,Kennedy, Alan R.,Tomkinson, Nicholas C. O.
, p. 6728 - 6740 (2018/06/26)
Treatment of homoallylic N-tosyl amines or allylic N-tosyl hydroxylamines with 1.5 equiv of a malonoyl peroxide provides a stereoselective method to access functionalized pyrrolidines and isoxazolidines. This metal free alkene oxyamination proceeds in 50-
New Prenylamine analogues: synthesis and Ca2+-entry blocking activity
Caldirola, PM,Goot, H van der,Timmerman, H
, p. 571 - 579 (2007/10/02)
The synthesis of a series of diphenylalkylamine derivatives related to prenylamine is reported.The amphetamine group in the prenylamine structure was replaced by other moieties.In addition to substitutions in the aromatic rings, heteroatoms such as sulphur and oxygen were introduced in the chain.The calcium-entry blocking activity was assayed in binding experiments on a guinea-pig brain membrane preparation by displacing -nitrendipine.
Hybrid Cholecystokinin-A Antagonists Based on Molecular Modelling of Lorglumide and L-364,718
Bent, Arie van der,Blommaert, Armand G. S.,Melman, Caroline T. M.,IJzerman, Adriaan P.,Wijngaarden, Ineke van,Soudijn, Willem
, p. 1042 - 1049 (2007/10/02)
A series of novel nonpeptide cholecystokinin-A (CCK-A) antagonists have been synthesized.Designed on the basis of the structural homology between lorgumide and L-364,718, as investigated with molecular modeling, these compounds constitute a link between the N-acylglutamic acid and 3-amino-5-phenyl-1,4-benzodiazepin-2-one derived antagonists.The prepared compounds were tested in vitro as antagonists of the binding of -(+/-)-L-364,718 and -CCK-8(S) to rat pancreas and guinea pig brain membranes, respectively.All compounds proved to be selective for the(peripheral) CCK-A receptor, the most potent analogue, 6, having a Ki value of 90 nM.The structure-activity profile of the series of hybrid compounds relates closest to that of the N-acylglutamic acid derived antagonists.
