124941-87-3Relevant academic research and scientific papers
Pillar[5]arene-based [3]rotaxanes: Convenient construction via multicomponent reaction and pH responsive self-assembly in water
Ye, Junmei,Zhang, Runmiao,Yang, Wenjuan,Han, Ying,Guo, Hao,Xie, Ju,Yan, Chaoguo,Yao, Yong
, p. 1550 - 1553 (2020)
Four pillar[5]arene based [3]rotaxanes (1-4) involving two 1,4-diethoxypillar[5]arene (DEP5) rings and a dumbbell-shaped component were successfully synthesized. The dumbbell-shape molecules contain one longer bridge, two triazole sites and two multicompo
Construction and investigation of photo-switch property of azobenzene-bridged pillar[5]arene-based [3]rotaxanes
Chong, Hui,Nie, Cuiyun,Wang, Lihong,Wang, Sicong,Han, Ying,Wang, Yang,Wang, Chengyin,Yan, Chaoguo
, p. 57 - 61 (2020/12/21)
Series of azobenzene-bridged pillar[5]arene-based [3]rotaxanes with different alkyl chain length of guest molecules were constructed by threading-endcapping method with alkylenetriazole as axile and tetrahydrochromene as endcapping group. The encapsulation of pillar[5]arenes were proved by high-resolution mass, 1H NMR and NOESY spectra. The photo-responsive property were examined by irradiation of the synthesized [3]rotaxanes with 365 nm and blue light LED, which caused trans to cis and cis to trans isomerization, respectively. Irradiation of corresponding model guest compounds without pillar[5]arene encapsulation resulted in near completely trans to cis and cis to trans isomerization, indicating the existence of pillar[5]arenes is the determining factor for the comprised photo isomerization efficiency.
COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
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Paragraph 0055; 0060, (2022/01/03)
The present invention relates to compounds of formula (I) as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the present disclosure, and their use as a medicament, in particular for the treatment of ne
Modification of a promiscuous inhibitor shifts the inhibition from γ-secretase to FLT-3
Amombo, Ghislaine Marlyse Okala,Kramer, Thomas,Lo Monte, Fabio,Goering, Stefan,Fach, Matthias,Smith, Steven,Kolb, Stephanie,Schubenel, Robert,Baumann, Karlheinz,Schmidt, Boris
supporting information, p. 7634 - 7640 (2013/02/21)
The inhibition of FLT-3 activity is an interesting target for the treatment of acute myeloid leukemia (AML). The serendipitous identification of FLT-3 inhibitors from a CK1/γ-secretase programme provided compounds with dual inhibitory activity. We analyzed the structure-activity relationship of these inhibitors and derivatized them to arrive at compounds with reduced impact on γ-secretase activity and enhanced FLT-3 inhibition.
Identification of 2-arylbenzimidazoles as potent human histamine H4 receptor ligands
Lee-Dutra, Alice,Arienti, Kristen L.,Buzard, Daniel J.,Hack, Michael D.,Khatuya, Haripada,Desai, Pragnya J.,Nguyen, Steven,Thurmond, Robin L.,Karlsson, Lars,Edwards, James P.,Breitenbucher, J. Guy
, p. 6043 - 6048 (2007/10/03)
A series of 2-arylbenzimidazoles was synthesized and found to bind with high affinity to the human histamine H4 receptor. Structure-activity relationships were investigated through library preparation and evaluation as well as traditional medicinal chemistry approaches, leading to the discovery of compounds with single-digit nanomolar affinity for the H4 receptor.
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.
