58026-13-4Relevant academic research and scientific papers
PHENANTHRENE AMPK ACTIVATOR COMPOUNDS, COMPOSITIONS, METHODS AND USES THEREOF
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, (2020/11/30)
The present invention relates to a compound having general formula I for use in the activation of AMPK. A composition comprising said compound for use in the activation of AMPK is also provided.
DIRECT AMPK ACTIVATOR COMPOUNDS
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, (2019/12/25)
The present invention relates to a compound having general formula I for use in the activation of AMPK. A composition comprising said compound for use in the activation of AMPK is also provided. Said compounds are 9,10 dihydrophenanthrenes, in particular selected from the group consisting of: (i) Lusianthridin i.e. 7- Methoxy-9,10-dihydrophenanthrene-2,5-diol, (ii) 7-Methoxy-9,10- dihydrophenanthrene-2,3,5-triol, (iii) 9,10-dihydrophenanthrene-2,5- diol, (iv) 9,10-Dihydrophenanthrene-2,4,7-triol (v) 9,10-Dihydro-7- methoxy-3,5-phenanthrenediol, and the activation of AMPK improves the condition, disorder, or disease related to cardiometabolic health, obesity, type 2 diabetes, non-alcoholic fatty liver disease, cardiovascular disease, and cancer.
Naturally occurring Batatasins and their derivatives as α-glucosidase inhibitors
Hu, Wei-Ping,Cao, Guo-Dong,Zhu, Jin-Hua,Li, Jia-Zhong,Liu, Xiu-Hua
, p. 82153 - 82158 (2015/10/12)
Batatasins are endogenous plant hormones found in yams and other related plant species. These plants are widely consumed as botanical dietary supplements in many parts of the world. This study investigated the inhibitory effects and mechanisms of Batatasin I, III, IV, V against α-glucosidase regarding their antidiabetic activities. The results revealed that Batatasin I, III, IV inhibited α-glucosidase in a reversible and noncompetitive manner, with IC50 values of 2.55, 1.89 and 2.52 mM respectively, while Batatasin V completely abolished its inhibitory activity even at the highest concentrations tested. Furthermore, a class of Batatasin-derived compounds with different substitution patterns was synthesized and subjected to the assay to clarify the structure-activity relationships, which suggested that the hydroxyl at the C-2′ position may play a significant role in improving the inhibitory activities. Their probable binding modes and the specificity of the binding sites were studied using molecule docking simulation. It was concluded that Batatasins, especially Batatasin III and IV, are promising α-glucosidase inhibitors, which therefore could be used as functional food to alleviate postprandial hyperglycemia and as potential candidates for the development of antidiabetic agents.
Two approaches to the aromatic core of the aminonaphthoquinone antibiotics
Nawrat, Christopher C.,Palmer, Leoni I.,Blake, Alexander J.,Moody, Christopher J.
, p. 5587 - 5603 (2013/07/26)
Two complementary approaches are presented for the synthesis of the quinone chromophores of the naphthoquinone ansamycins and related natural products. The first involves the use of an improved protocol for the manganese(III) acetate mediated cyclization of 5-aryl-1,3-dicarbonyl compounds to β-naphthols, leading to the simple, scalable preparation of building blocks suitable for the synthesis of naturally occurring aminonaphthoquinones. The second approach involves the Diels-Alder reaction of a series of new, ester-containing Danishefsky-type dienes with N-protected aminobenzoquinones to allow more expeditious access to similar intermediates.
Dendrimer disassembly in the gas phase: A cascade fragmentation reaction of frechet dendrons
Baytekin, Bilge,Tank Bavtekin,Hahn, Uwe,Reckien, Werner,Kirchner, Barbara,Schalley, Christoph A.
supporting information; experimental part, p. 7139 - 7149 (2010/03/05)
The mass spectrometry characterization of Frechet-type dendrons is reported. In order to provide the charges necessary for electrospray ionization, dendrons bearing an OH group at the focal point can be deprotonated and observed in the negative ion mode.
Dihydrostilbenes of Cannabis. Synthesis of Canniprene
Crombie, Leslie,Jamieson, Sally V.
, p. 1467 - 1476 (2007/10/02)
Canniprene (10) is synthesised via reaction of a phenolate-anion ylide with a benzyl-protected aldehyde.Benzoylation, followed by hydrogenation and hydrogenolysis of the resulting stilbene, leads to a half-benzoylated bibenzyl which is converted into its O-dimethylprop-2-ynyl derivative.Semi-hydrogenation, Claisen rearrangement, and debenzoylation gives canniprene.In a second synthesis the prenylated (3-methylbut-2-enylated) and benzyl-protected ring-B section is made first and converted by Wittig reaction into a dibenzyl-protected stilbene.The stilbene is reduced and the benzyl groups removed in one step, without affecting the prenyl group, by sodium in butanol: magnesium in methanol is capable of stilbene reduction without debenzylation.This practical synthesis proceeds in 19 percent overall yield from the dimethylprop-2-ynyl ether of isovanillin (14) and is applicable to isotopelabelling.The use of p-bromophenacyl (PBP) ether and methoxyethoxymethyl (MEM) ether protection as the basis for canniprene synthesis is also considered.Other bibenzyls relevant to the natural products of Cannabis are made and the methylated chroman (37) derived from canniprene is also synthesised.
