474009-16-0Relevant articles and documents
AMPK ACTIVATORS
-
Paragraph 00254, (2021/11/26)
This disclosure is directed, at least in part, to AMPK activators useful for the treatment of conditions or disorders associated with AMPK. In some embodiments, the condition or disorder is associated with the gut-brain axis. In some embodiments, condition or disorder is associated with systemic infection and inflammation from having a leaky gut barrier. In some embodiments, the AMPK activators are gut-restricted compounds. In some embodiments, the AMPK activators are agonists or partial agonists.
Phenolic bis-styrylbenzenes as β-amyloid binding ligands and free radical scavengers
Flaherty, Daniel P.,Kiyota, Tomomi,Dong, Yuxiang,Ikezu, Tsuneya,Vennerstrom, Jonathan L.
supporting information; experimental part, p. 7992 - 7999 (2011/03/19)
Starting from bisphenolic bis-styrylbenzene DF-9 (4), β-amyloid (Aβ) binding affinity and specificity for phenolic bis-styrylbenzenes, monostyrylbenzenes, and alkyne controls were determined by fluorescence titration with β-amyloid peptide Aβ1-40 and a fluorescence assay using APP/PS1 transgenic mouse brain sections. Bis-styrylbenzene SAR is derived largely from work on symmetrical compounds. This study is the first to describe Aβ binding data for bis-styrylbenzenes unsymmetrical in the outer rings. With one exception, binding affinity and specificity were decreased by adding and/or changing the substitution pattern of phenol functional groups, changing the orientation about the central phenyl ring, replacing the alkene with alkyne bonds, or eliminating the central phenyl ring. The only compound with an Aβ binding affinity and specificity comparable to 4 was its 3-hydroxy regioisomer 8. Like 4, 8 crossed the blood-brain barrier and bound to Aβ plaques in vivo. By use of a DPPH assay, phenol functional groups with para orientations seem to be a necessary, but insufficient, criterion for good free radical scavenging properties in these compounds.
Asymmetric synthesis of isobenzofuranone derivatives and their unique character as protein kinase Cα (PKCα) activators
Hirai, Go,Ogoshi, Yosuke,Ohkubo, Megumi,Tamura, Yuki,Watanabe, Toru,Shimizu, Tadashi,Sodeoka, Mikiko
scheme or table, p. 3609 - 3612 (2009/09/28)
Efficient enantio-selective synthesis of conformationally constrained diacylglycerol analogues, 7-substituted isobenzofuranone derivatives, originally developed by us as PKCα ligands, was achieved by asymmetric dihydroxylation and γ-lactone formation via
Total synthesis of (-)-amathaspiramide F
Sakaguchi, Kazuhiko,Ayabe, Miki,Watanabe, Yusuke,Okada, Takuya,Kawamura, Kazushige,Shiada, Tetsuro,Ohfune, Yasufumi
supporting information; experimental part, p. 5449 - 5452 (2009/06/20)
(Chemical Equation Presented) The stereoselective total synthesis of the marine alkaloid (-)-amathaspiramide F (1) was achieved from the α-hydoxy-α-ethynylsilane 2. The crucial steps in this synthesis involved not only the enolate Claisen rearrangement of
TROPAN COMPOUND
-
Page/Page column 49, (2010/11/27)
The conventional anticholinergic drugs for administration through inhalation have been considered to have the possibility of aggravating dysuria associated with prostatic hyperplasia mediated by blood, and it has been demanded that the conventional anticholinergic drugs for administration through inhalation will have to show reduced side effects or adverse ractions. The present invention relates to a compound represented by the general formula (I): (wherein A represents; and R1, R2, R3 and R1 each a hydrogen atom or a substituent; R5 is a substituent; X- is an anion;the symbol: denotes an exo-form or endo-form, or their mixture), its salt or solvation product thereof. They are useful as a prophylactic and/or therapeutic agent with reduced side effects or adverse reactions for the diseases mediated by the muscarinic receptor.
