65136-48-3Relevant academic research and scientific papers
The neuronal calcium ion channel activity of constrained analogues of MONIRO-1
Bispat, Anjie,Cardoso, Fernanda C.,Duggan, Peter J.,Geoffroy, Chloe,Lewis, Richard J.,Marliac, Marie-Adeline,Schmit, Matthieu,Tuck, Kellie L.
, (2020/07/28)
Structural modifications of the neuronal calcium channel blocker MONIRO-1, including constraining the phenoxyaniline portion of the molecule and replacing the guanidinium functionality with tertiary amines, led to compounds with significantly improved aff
Preparation and applications of phenylquinolinone-based and flavone-based derivative
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, (2019/01/10)
The present invention relates to a phenylquinolinone-based and flavone-based derivative and a preparation method thereof, wherein the derivative is a histamine H3 receptor antagonist, can protect andrestore the normal function of central nervous system, e
Discovery of novel benzofuran-based compounds with neuroprotective and immunomodulatory properties for Alzheimer's disease treatment
Montanari, Serena,Mahmoud, Ali Mokhtar,Pruccoli, Letizia,Rabbito, Alessandro,Naldi, Marina,Petralla, Sabrina,Moraleda, Ignacio,Bartolini, Manuela,Monti, Barbara,Iriepa, Isabel,Belluti, Federica,Gobbi, Silvia,Di Marzo, Vincenzo,Bisi, Alessandra,Tarozzi, Andrea,Ligresti, Alessia,Rampa, Angela
, p. 243 - 258 (2019/06/14)
To address the multifactorial nature of Alzheimer's Disease (AD), a multi-target-directed ligand approach was herein developed. As a follow-up of our previous studies, a small library of newly designed 2-arylbenzofuran derivatives was evaluated towards ch
Inhibition of N-type calcium channels by fluorophenoxyanilide derivatives
Gleeson, Ellen C.,Graham, Janease E.,Spiller, Sandro,Vetter, Irina,Lewis, Richard J.,Duggan, Peter J.,Tuck, Kellie L.
, p. 2030 - 2045 (2015/05/04)
A set of fluorophenoxyanilides, designed to be simplified analogues of previously reported ω-conotoxin GVIA mimetics, were prepared and tested for N-type calcium channel inhibition in a SH-SY5Y neuroblastoma FLIPR assay. N-type or Cav2.2 channe
FUSED OXAZOLES and THIAZOLES AS HISTAMINE H3- RECEPTOR LIGANDS
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Page/Page column 93-94, (2008/06/13)
The present invention relates to compounds comprising fused oxazole or thiazole derivatives of formula (I), processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as H3-receptor ligands, wherein A is a cyclic amine which is linked to the propylene group via an amino nitrogen; B is selected from the group consisting of heteroaryl, 5-8-membered heterocycloalkyl, 5-8-membered cycloalkyl; X is either N or CH; Y is either O or S.
Synthesis of (aryloxy)alkylamines. 1. Novel antisecretory agents with H+K+-ATPase inhibitory activity
Sanfilippo,Urbanski,Press,Hajos,Shriver,Scott
, p. 1778 - 1785 (2007/10/02)
A series of heterocyclic (aryloxy)alkylamines of structures II and III were prepared and found to possess gastric antisecretory activity. Of the variety of substituted thiazoles, benzoxazoles, and benzothiazoles prepared, thiazole 18, benzoxazole 32, and benzothiazole 47 exhibited gastric antisecretory potency comparable to that of ranitidine in vivo in the pylorous ligated rat model. In an isolated rabbit parietal system, the series of thiazoles, benzoxazoles, and benzothiazoles also demonstrated similar potency to that of ranitidine toward the inhibition of both histamine-stimulated and dcAMP-stimulated uptake of amino[14C]pyrine. These compounds inhibited the H+K+-sensitive ATPase enzyme in isolated gastric microsomes. A direct correlation existed between inhibition of 14C uptake, in vivo antisecretory activity, and inhibition of the H+K+-ATPase enzyme. The more potent antisecretory compounds 18, 32 and 47 were also the more potent enzyme inhibitors. These data suggest that the mechanism responsible for the observed in vitro and in vivo gastric antisecretory activity, in these series of compounds, is a consequence of the inhibition of the H+K+-sensitive ATPase enzyme.
