20366-86-3Relevant academic research and scientific papers
Design, synthesis and ability of non-gold complexed substituted purine derivatives to inhibit LPS-induced inflammatory response
Wang, Xuebao,Han, Chao,Wu, Kaiqi,Luo, Lu,Wang, Yu,Du, Xuze,He, Qin,Ye, Faqing
, p. 10 - 21 (2018/03/01)
In order to study the anti-inflammatory activity of novel 6-substituted and 6,9-disubstituted purine derivatives, 20 compounds, L1–10 and W1–10, derived from purine and lacking a gold complex were designed, synthesized and their anti-inflammatory activity was screened. LPS-induced TNF-α, IL-1β, IL-6, PGE2, NO, COX-2 and iNOS mRNA were evaluated, and western blot and NF-κB p65 translocation assay were performed in RAW 264.7 macrophages. Furthermore, carrageenan-induced hind paw edema experiments were performed in mice. Compound L1, L4, W2, and W4 markedly exerted a dose-dependent inhibition of TNF-α, IL-1β, IL-6 and PGE2 release induced by LPS in RAW 264.7 macrophages. Moreover, these compounds strongly inhibited LPS-induced NO, COX-2 and iNOS mRNA in the same cells. Anti-inflammatory activity tests in vivo showed that L1 and L4 were more effective than Au(L3)(PPh3), a known anti-inflammatory agent, at 2–5 h, and W4 was the most effective at 3–5 h after dosing. Thus, W2, W4, and L1, L4, could effectively inhibit LPS-induced inflammatory response in vitro and in vivo suggesting a promising role as anti-inflammatory agents.
6-substituted-9H-purine derivative and preparation method and application thereof
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Paragraph 0042; 0043; 0044; 0046; 0048; 0049; 0051; 0068, (2017/08/29)
The invention discloses a 6-substituted-9H-purine derivative and a preparation method and application thereof. The derivative has the structure shown as the formula (I). In the formula (I), R is selected from one of pyrrolidiny, furan-2-methyl, benzenesulfonyl, and substituted or unsubstituted phenyl or benzyl, wherein a substituent on phenyl or benzyl is independently selected from one or more of C1-C4 alkoxy, C1-C4 alkyl, hydroxyl, halogen and a group shown in the description, and R4 is independently selected from H or alkyl-substituted benzyl. It is shown in the experimental results that compared with 6-benzyl purine compound complex gold ions (an inhibitor 3), the 6-substituted-9H-purine derivative is higher in inhibition ratio of inflammatory factors and has better anti-inflammatory activity. The 6-substituted-9H-purine derivative has the potential as an anti-inflammatory medicine.
9-subsituted-N-(2-chlorobenzyl)purine-6-amine derivative, as well as preparation method and application thereof
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Paragraph 0047; 0048; 0050, (2017/08/28)
The invention discloses a 9-subsituted-N-(2-chlorobenzyl)purine-6-amine derivative. The structure of the derivative is shown in a formula (I), where R is selected from a hydrogen atom, a C1-C4 alkyl group and a substituted or unsubstituted benzyl group, and a substituent on the benzyl group is one or more independently selected from halogen, -CF3, a C1-C4 alkoxy group, a C1-C4 alkyl group and a nitro group; R4 is a substituted or unsubstituted phenyl group or benzyl group, and a substituent on the phenyl group or the benzyl group is one or more of halogen and a methoxy group. Compared with a 6-benyl adenine compound complex gold ion (inhibitor 3), the 9-subsituted-N-(2-chlorobenzyl)purine-6-amine derivative is proved by testing results to have the advantages of higher inflammation factor inhibition rate, higher anti-inflammation activity and potential for use as an anti-inflammation medicament. (The formula (I) is shown in the description.).
Diverse in vitro and in vivo anti-inflammatory effects of trichlorido-gold(III) complexes with N6-benzyladenine derivatives
K?ikavová, Radka,Ho?ek, Jan,Suchy, Pavel,Van?o, Ján,Trávní?ek, Zdeněk
, p. 92 - 99 (2014/03/21)
A series of gold(III) complexes involving differently substituted derivatives of a plant hormone N6-benzyladenine (HL1-5) is reported. The complexes have the general formula [Au(HL1-5)Cl3] a?nH2O (n = 0 for 1, 3-5; and n = 1 for 2),
Method for treating disease or condition susceptible to amelioration by AMPK activators and compounds of formula which are useful to activate AMP-activated protein kinase (AMPK)
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Paragraph 0051-0052, (2014/10/16)
The present invention relates to a method for treating disease or condition susceptible to amelioration by AMPK activators and compounds of formula which are useful to activate AMP-activated protein kinase (AMPK) and the use of the compounds in the prevention or treatment of disease, including pre-diabetes, type 2 diabetes, syndrome X, metabolic syndrome and obesity.
Preparation and biological activity of 6-benzylaminopurine derivatives in plants and human cancer cells
Dolezal, Karel,Popa, Igor,Krystof, Vladimir,Spichal, Lukas,Fojtikova, Martina,Holub, Jan,Lenobel, Rene,Schmuelling, Thomas,Strnad, Miroslav
, p. 875 - 884 (2007/10/03)
To study the structure-activity relationships of aromatic cytokinins, the cytokinin activity at both the receptor and cellular levels, as well as CDK inhibitory and anticancer properties of 38 6-benzylaminopurine (BAP) derivatives were compared in various
