Characterization of novel furan compounds on the basis of their radical scavenging activity and cytoprotective effects against glutamate- and lipopolysaccharide-induced insults.


:There is increasing evidence indicating that free radicals and oxygenases such as cyclooxygenase (COX) and lipoxygenase (LOX) are related to the onset and development of neurodegenerative diseases. In order to prevent and/or delay these diseases, the use of radical-scavenging antioxidants and inhibitors against oxygenases has received much attention. In the present study, we examined the radical-scavenging activity and cytoprotective effects of some novel furan compounds with potent inhibitory activity against oxygenases such as COX-1, COX-2, and 5-LOX. The radical-scavenging activity was assessed by studying the bleaching of beta-carotene by free radicals generated from an azo initiator. In this assay system, the rate constants for scavenging peroxyl radicals by furan S and furan L was estimated to be 2 x 10(4) and 3 x 10(4) M(-1) s(-1), respectively. We also investigated the cytoprotective effects of these compounds against cell death induced by several toxins. We found that the furan compounds exhibited cytoprotective effects against PC12 cell death induced by linoleic acid hydroperoxide, primary neuronal cell death induced by glutamate, and cell death induced by lipopolysaccharide. These results suggest the beneficial effects of the furan compounds against disorders related to glutamate and lipopolysaccharide.


Bioorg Med Chem


Nishio K,Fukuhara A,Omata Y,Saito Y,Yamaguchi S,Kato H,Yoshida Y,Niki E




Has Abstract


2008-12-15 00:00:00














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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Hallinan EA,Hagen TJ,Tsymbalov S,Stapelfeld A,Savage MA

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    abstract::2-Phenyl-9-benzyl-8-azapurines, bearing at the 6 position an amido group interposed between the 8-azapurine moiety and an alkyl or a substituted phenyl group, have been synthesised and assayed as ligands for adenosine receptors. All the compounds show high affinity for the A(1) adenosine receptor, and many of them als...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Giorgi I,Leonardi M,Pietra D,Biagi G,Borghini A,Massarelli I,Ciampi O,Bianucci AM

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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Geldenhuys WJ,Malan SF,Murugesan T,Van der Schyf CJ,Bloomquist JR

    更新日期:2004-04-01 00:00:00

  • Scutione, a new bioactive norquinonemethide triterpene from Maytenus scutioides (Celastraceae).

    abstract::Scutione (1), a new norquinonemethide triterpene with a netzahualcoyene type skeleton, has been isolated from the root bark of Maytenus scutioides (Celastraceae) by bioactivity-directed fractionation. The structure of 1 has been elucidated by means of 1H and 13C NMR spectroscopic studies, including 1H-13C heteronuclea...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: González AG,Alvarenga NL,Ravelo AG,Bazzocchi IL,Ferro EA,Navarro AG,Moujir LM

    更新日期:1996-06-01 00:00:00

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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Arnó M,Betancur-Galvis L,González MA,Sierra J,Zaragozá RJ

    更新日期:2003-07-17 00:00:00

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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Lee CS,Allwine DA,Barbachyn MR,Grega KC,Dolak LA,Ford CW,Jensen RM,Seest EP,Hamel JC,Schaadt RD,Stapert D,Yagi BH,Zurenko GE,Genin MJ

    更新日期:2001-12-01 00:00:00

  • Structural insights into binding of inhibitors to soluble epoxide hydrolase gained by fragment screening and X-ray crystallography.

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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Amano Y,Yamaguchi T,Tanabe E

    更新日期:2014-04-15 00:00:00

  • 2-(2-Bromophenyl)-formononetin and 2-heptyl-formononetin are PPARγ partial agonists and reduce lipid accumulation in 3T3-L1 adipocytes.

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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Andersen C,Kotowska D,Tortzen CG,Kristiansen K,Nielsen J,Petersen RK

    更新日期:2014-11-01 00:00:00

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    abstract::A series of new 4-amino-3-[3-[4-(2-methoxy or nitro phenyl)-1-piperazinyl] propyl]thio]-5-(substitutedphenyl)[1,2,4]triazoles 11a-t was synthesized in order to obtain compounds with high affinity and selectivity for 5-HT(1A) receptor over the alpha(1)-adrenoceptor. A series of isomeric 4-amino-2-[3-[4-(2-methoxy or ni...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Sarvà MC,Romeo G,Guerrera F,Siracusa M,Salerno L,Russo F,Cagnotto A,Goegan M,Mennini T

    更新日期:2002-02-01 00:00:00

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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Toropov AA,Benfenati E

    更新日期:2006-04-15 00:00:00

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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Anami Y,Sakamaki Y,Itoh T,Inaba Y,Nakabayashi M,Ikura T,Ito N,Yamamoto K

    更新日期:2015-11-15 00:00:00

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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Liu T,Joo SH,Voorhees JL,Brooks CL,Pei D

    更新日期:2009-02-01 00:00:00

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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


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    更新日期:2010-09-01 00:00:00

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    authors: Tantravedi S,Chakraborty S,Shah NH,Fishbein JC,Hosmane RS

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    更新日期:2009-01-01 00:00:00

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    pub_type: 杂志文章


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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


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    更新日期:2013-07-15 00:00:00

  • Pyrrolomycins as antimicrobial agents. Microwave-assisted organic synthesis and insights into their antimicrobial mechanism of action.

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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Wone DW,Rowley JA,Garofalo AW,Berkman CE

    更新日期:2006-01-01 00:00:00

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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


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    更新日期:2009-12-01 00:00:00

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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Berne S,Kovačič L,Sova M,Kraševec N,Gobec S,Križaj I,Komel R

    更新日期:2015-08-01 00:00:00

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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Chen W,Shen S,Dong L,Zhang J,Yang Q

    更新日期:2018-01-15 00:00:00

  • Substituted thiophene-anthranilamides as potent inhibitors of human factor Xa.

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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Kochanny MJ,Adler M,Ewing J,Griedel BD,Ho E,Karanjawala R,Lee W,Lentz D,Liang AM,Morrissey MM,Phillips GB,Post J,Sacchi KL,Sakata ST,Subramanyam B,Vergona R,Walters J,White KA,Whitlow M,Ye B,Zhao Z,Shaw KJ

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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Iijima H,Kimura K,Sakai T,Uchimura A,Shimizu T,Ueno H,Natori T,Koezuka Y

    更新日期:1998-10-01 00:00:00

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    abstract::In this article, we report our efforts towards improving in vitro human clearance in a series of 5-azaquinazolines through a series of C4 truncations and C2 expansions. Extensive DMPK studies enabled us to tackle high Aldehyde Oxidase (AO) metabolism and unexpected discrepancies in human hepatocyte and liver microsoma...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Degorce SL,Aagaard A,Anjum R,Cumming IA,Diène CR,Fallan C,Johnson T,Leuchowius KJ,Orton AL,Pearson S,Robb GR,Rosen A,Scarfe GB,Scott JS,Smith JM,Steward OR,Terstiege I,Tucker MJ,Turner P,Wilkinson SD,Wrigley GL,

    更新日期:2020-12-01 00:00:00

  • Novel trans-2-aryl-cyclopropylamine analogues as potent and selective dipeptidyl peptidase IV inhibitors.

    abstract::A series of trans-2-aryl-cyclopropylamine derived compounds were synthesized and evaluated their biological activities against DPP-IV. The structure-activity relationships (SAR) led to the discovery of novel series of DPP-IV inhibitors, having IC(50) values of <100 nM with excellent selectivity over the closely relate...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Tsai TY,Hsu T,Chen CT,Cheng JH,Yeh TK,Chen X,Huang CY,Chang CN,Yeh KC,Hsieh SH,Chien CH,Chang YW,Huang CH,Huang YW,Huang CL,Wu SH,Wang MH,Lu CT,Chao YS,Jiaang WT

    更新日期:2009-03-15 00:00:00

  • Transition state analogue inhibitors of protozoan nucleoside hydrolases.

    abstract::Protozoan parasites are unable to synthesize purines de novo and must rely on purine salvage pathways for their requirements. Nucleoside hydrolases, which are not found in mammals, function as key enzymes in purine salvage in protozoa. Inhibition of these enzymes may disrupt purine supply and specific inhibitors are p...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Furneaux RH,Schramm VL,Tyler PC

    更新日期:1999-11-01 00:00:00