当前位置： SCI文献检索 > BIOORGANIC & MEDICINAL CHEMISTRY LETTERS期刊下所有文献 > Antitrypanosomal and antioxidant properties of 4-hydroxycoumarins derivatives.

Antitrypanosomal and antioxidant properties of 4-hydroxycoumarins derivatives.

Abstract：

:In the present communication we prepared a series of six 4-hydroxycoumarin derivatives, isosters of quercetin, recognized as an antioxidant natural compound, with the aim of evaluating the antitrypanosomal activity against Trypanosoma cruzi, the parasite responsible for Chagas disease, and the antioxidant properties. We have used the 4-hydroxycoumarin moiety (compound 1) as the molecular template for the synthesis of compounds 2-7. These derivates have shown moderate trypanocidal activity. However they have been proved to be good antioxidants. In particular compound 7 is the most active antioxidant and it is, therefore, a potential candidate for a successful employment in conditions characterized by free radicals overproduction.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Pérez-Cruz F,Serra S,Delogu G,Lapier M,Maya JD,Olea-Azar C,Santana L,Uriarte E

doi

10.1016/j.bmcl.2012.07.013

subject

Has Abstract

pub_date

2012-09-01 00:00:00

pages

5569-73

issue

17

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(12)00880-3

journal_volume

22

pub_type

杂志文章

相关文献

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS文献大全
  • Identification of peptidomimetic HTLV-I protease inhibitors containing hydroxymethylcarbonyl (HMC) isostere as the transition-state mimic.

    abstract：:Towards the development of chemotherapy for the infection by human T-cell leukemia virus type I (HTLV-I), we have established evaluation systems for HTLV-I protease (PR) inhibitors using both recombinant and chemically synthesized HTLV-I PRs. Newly synthesized substrate-based inhibitors containing hydroxymethylcarbony...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2004.09.034

    authors： Maegawa H,Kimura T,Arii Y,Matsui Y,Kasai S,Hayashi Y,Kiso Y

    更新日期：2004-12-06 00:00:00

  • Conformationally restricted analogs of Combretastatin A-4 derived from SU5416.

    abstract：:A series of compounds originally derived from the vascular endothelial growth factor receptor tyrosine kinase inhibitor, SU5416, was synthesized and evaluated. The most potent compound in this series, compound 7, structurally resembles the potent anti-microtubule agent Combretastatin A-4, inhibited tubulin polymerizat...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2005.09.001

    authors： Li PK,Xiao Z,Hu Z,Pandit B,Sun Y,Sackett DL,Werbovetz K,Lewis A,Johnsamuel J

    更新日期：2005-12-15 00:00:00

  • Novel 1H-(benzimidazol-2-yl)-1H-pyridin-2-one inhibitors of insulin-like growth factor I (IGF-1R) kinase.

    abstract：:A novel class of 1H-(benzimidazol-2-yl)-1H-pyridin-2-one inhibitors of insulin-like growth factor I (IGF-1R) kinase is described. This report discusses the SAR of 4-(2-hydroxy-2-phenylethylamino)-substituted pyridones with improved IGF-1R potency. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2006.11.041

    authors： Wittman MD,Balasubramanian B,Stoffan K,Velaparthi U,Liu P,Krishnanathan S,Carboni J,Li A,Greer A,Attar R,Gottardis M,Chang C,Jacobson B,Sun Y,Hansel S,Zoeckler M,Vyas DM

    更新日期：2007-02-15 00:00:00

  • Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors.

    abstract：:A series of substituted 2-(aminoheteroaryl)-thiazole-5-carboxamide analogs have been synthesized as novel, potent inhibitors of the Src-family kinase p56Lck. Among them, compound 2 displayed superior in vitro potency and excellent in vivo efficacy. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2004.09.093

    authors： Chen P,Norris D,Das J,Spergel SH,Wityak J,Leith L,Zhao R,Chen BC,Pitt S,Pang S,Shen DR,Zhang R,De Fex HF,Doweyko AM,McIntyre KW,Shuster DJ,Behnia K,Schieven GL,Barrish JC

    更新日期：2004-12-20 00:00:00

  • Synthesis of novel lignan-like compounds and their antimicrobial activity.

    abstract：:Herein we report the preparation of 3,4-dibenzylfurans and some oxidized derivatives with lignan backbone. The compounds were prepared using the Friedel-Crafts reaction with BF3 etherate as catalyst, demethylation with iodocyclohexane, acetylation and oxidation reactions. The antimicrobial activity was evaluated throu...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2020.127413

    authors： Tufano I,Buommino E,Iesce MR,De Filippis A,Grieco P,Lembo F,DellaGreca M

    更新日期：2020-09-01 00:00:00

  • Synthesis and cytotoxic evaluation of novel ester-triazole-linked triterpenoid-AZT conjugates.

    abstract：:Betulinic acid and analogous naturally occurring triterpenoid acids were transformed into the corresponding propargyl esters and subsequently deployed as substrates for a click chemistry-mediated coupling with azidothymidine (AZT) en route to novel 1,2,3-triazole-tethered triterpenoid-AZT conjugates. Twelve new hybrid...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2014.09.079

    authors： Dang Thi TA,Kim Tuyet NT,Pham The C,Thanh Nguyen H,Ba Thi C,Doan Duy T,D'hooghe M,Van Nguyen T

    更新日期：2014-11-15 00:00:00

  • Investigations of the esterase, phosphatase, and sulfatase activities of the cytosolic mammalian carbonic anhydrase isoforms I, II, and XIII with 4-nitrophenyl esters as substrates.

    abstract：:The esterase, phosphatase, and sulfatase activities of carbonic anhydrase (CA, EC 4.2.1.1) isozymes, CA I, II, and XIII with 4-nitrophenyl esters as substrates was investigated. These enzymes show esterase activity with 4-nitrophenyl acetate as substrate, with second order rate constants in the range of 753-7706M(-1)s...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2008.03.012

    authors： Innocenti A,Scozzafava A,Parkkila S,Puccetti L,De Simone G,Supuran CT

    更新日期：2008-04-01 00:00:00

  • Design, synthesis and biological evaluation of potent NAD+-dependent DNA ligase inhibitors as potential antibacterial agents. Part 2: 4-amino-pyrido[2,3-d]pyrimidin-5(8H)-ones.

    abstract：:A series of 4-amino-pyrido[2,3-d]pyrimidin-5(8H)-ones were designed and synthesized as a novel class of inhibitors of NAD(+)-dependent DNA ligase that possess potency against Gram-positive bacteria. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2012.04.038

    authors： Wang T,Duncan L,Gu W,O'Dowd H,Wei Y,Perola E,Parsons J,Gross CH,Moody CS,Arends SJ,Charifson PS

    更新日期：2012-06-01 00:00:00

  • Respiratory syncytial virus fusion inhibitors. Part 4: optimization for oral bioavailability.

    abstract：:A series of benzimidazole-based inhibitors of respiratory syncytial virus (RSV) fusion were optimized for antiviral potency, membrane permeability and metabolic stability in human liver microsomes. 1-Cyclopropyl-1,3-dihydro-3-[[1-(4-hydroxybutyl)-1H-benzimidazol-2-yl]methyl]-2H-imidazo[4,5-c]pyridin-2-one (6m, BMS-433...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2006.11.063

    authors： Yu KL,Sin N,Civiello RL,Wang XA,Combrink KD,Gulgeze HB,Venables BL,Wright JJ,Dalterio RA,Zadjura L,Marino A,Dando S,D'Arienzo C,Kadow KF,Cianci CW,Li Z,Clarke J,Genovesi EV,Medina I,Lamb L,Colonno RJ,Yang Z,Kr

    更新日期：2007-02-15 00:00:00

  • Discovery of ML326: The first sub-micromolar, selective M5 PAM.

    abstract：:This Letter describes the further chemical optimization of the M5 PAM MLPCN probes ML129 and ML172. A multi-dimensional iterative parallel synthesis effort quickly explored isatin replacements and a number of southern heterobiaryl variations with no improvement over ML129 and ML172. An HTS campaign identified several ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2013.03.032

    authors： Gentry PR,Bridges TM,Lamsal A,Vinson PN,Smith E,Chase P,Hodder PS,Engers JL,Niswender CM,Daniels JS,Conn PJ,Wood MR,Lindsley CW

    更新日期：2013-05-15 00:00:00

  • Synthesis of rigid trichostatin A analogs as HDAC inhibitors.

    abstract：:New inhibitors of histone deacetylase (HDAC) have been synthesized and evaluated for their activity toward non small lung cancer cell line H661. Their design is based on indanone (or tetralone) systems leading to trichostatin A (TSA) analogs with limited conformational mobility. Molecular modelization at the AM1 level...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2006.07.080

    authors： Charrier C,Bertrand P,Gesson JP,Roche J

    更新日期：2006-10-15 00:00:00

  • Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.

    abstract：:A series of N1-activated C4-carboxy azetidinones was prepared and tested as inhibitors of human tryptase. The key stereochemical and functional features required for potency, serine protease specificity and aqueous stability were determined. From these studies compound 2, BMS-262084, was identified as a potent and sel...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(02)00688-1

    authors： Sutton JC,Bolton SA,Hartl KS,Huang MH,Jacobs G,Meng W,Ogletree ML,Pi Z,Schumacher WA,Seiler SM,Slusarchyk WA,Treuner U,Zahler R,Zhao G,Bisacchi GS

    更新日期：2002-11-04 00:00:00

  • Preparation, characterization, molecular modeling and in vitro activity of paclitaxel-cyclodextrin complexes.

    abstract：:Paclitaxel (PTX) was complexed with beta-cyclodextrin (1), 2,6-dimethyl-beta-cyclodextrin (2) and 2,3,6-trimethyl-beta-cyclodextrin (3). PTX-CYD complexes were characterized both at the solid and liquid states. Experimental findings are in agreement with molecular modeling analysis, which showed different PTX-CYD inte...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(02)00217-2

    authors： Alcaro S,Ventura CA,Paolino D,Battaglia D,Ortuso F,Cattel L,Puglisi G,Fresta M

    更新日期：2002-06-17 00:00:00

  • Synthesis of hydrophilic and flexible linkers for peptide derivatization in solid phase.

    abstract：:Four N-Fmoc protected polyoxyethylene-based amino acid type linkers were designed and synthesized for peptide derivatization in solid phase. Three of them were obtained in a crystalline form. The crystallized linkers can be stored at 4 degrees C for 2 years without significant decomposition. Protocols for biotinylatio...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2003.09.067

    authors： Song A,Wang X,Zhang J,Marík J,Lebrilla CB,Lam KS

    更新日期：2004-01-05 00:00:00

  • 4-Alkyl and 4,4'-dialkyl 1,2-bis(4-chlorophenyl)pyrazolidine-3,5-dione derivatives as new inhibitors of bacterial cell wall biosynthesis.

    abstract：:Over 195 4-alkyl and 4,4-dialkyl 1,2-bis(4-chlorophenyl)pyrazolidine-3,5-dione derivatives were synthesized, utilizing microwave accelerated synthesis, for evaluation as new inhibitors of bacterial cell wall biosynthesis. Many of them demonstrated good activity against MurB in vitro and low MIC values against gram-pos...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2005.03.058

    authors： Kutterer KM,Davis JM,Singh G,Yang Y,Hu W,Severin A,Rasmussen BA,Krishnamurthy G,Failli A,Katz AH

    更新日期：2005-05-16 00:00:00

  • Progress in the discovery of small molecule modulators of the Cys-loop superfamily receptors.

    abstract：:The vertebrate Cys-loop family of ligand-gated ion channels (LGICs) are comprised of nicotinic acetylcholine (nAChR), serotonin type 3 (5-HT3R), γ-aminobutyric acid (GABAAR), and glycine (GlyR) receptors. Here, we review efforts to discover selective small molecules targeting one or more Cys-loop receptors, with a foc...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章,评审

    doi：10.1016/j.bmcl.2017.04.073

    authors： Sparling BA,DiMauro EF

    更新日期：2017-08-01 00:00:00

  • Design and synthesis of a novel class of nucleotide analogs with anti-HCMV activity.

    abstract：:A novel class of cyclic nucleotide analogs has shown anti-HCMV activity. The synthesis as well as structure-activity relationship studies are presented. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(98)00648-9

    authors： Nguyen-Ba P,Lee N,Mitchell H,Chan L,Quimpère M

    更新日期：1998-12-15 00:00:00

  • Novel 1,3,4-oxadiazole thioether derivatives containing flexible-chain moiety: Design, synthesis, nematocidal activities, and pesticide-likeness analysis.

    abstract：:Seventy-two novel 1,3,4-oxadiazole thioether derivatives containing different flexible-chain moieties were designed and synthesized. The nematicidal activities of all the title compounds were evaluated, and some compounds showed excellent nematicidal activities against citrus nematodes. The compounds 15, 16, 18, 27, 4...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2020.127028

    authors： Chen J,Wei C,Wu S,Luo Y,Wu R,Hu D,Song B

    更新日期：2020-04-15 00:00:00

  • Synthesis, thermal stability, antimalarial activity of symmetrically and asymmetrically substituted tetraoxanes.

    abstract：:Symmetrically and asymmetrically substituted 1,2,4,5-tetraoxanes were synthesized by the oxidative system H(2)O(2)/TFE in presence of MeReO(3) as a catalyst. All of the synthesized compounds were characterized spectroscopically, and evaluated for cytotoxicity, and antimalarial activity. Several of these tetraoxanes ex...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2007.12.069

    authors： Atheaya H,Khan SI,Mamgain R,Rawat DS

    更新日期：2008-02-15 00:00:00

  • Inhibition of HIV-1 infection by synthetic peptide analogues derived from the NH(2)-Terminal extracellular region of GPR1.

    abstract：:Several shortened peptide analogues of the N-terminal domain of GPR1, an orphan G protein-coupled receptor (GPCR), were prepared and their anti-HIV-1 activities were evaluated. Some of the prepared compounds, especially sulfated derivatives, showed potent inhibitory activity against a broad range of HIV-1, including T...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(01)00503-0

    authors： Ikeda K,Konishi K,Sato M,Hoshino H,Tanaka K

    更新日期：2001-10-08 00:00:00

  • Discovery of core-structurally novel PTP1B inhibitors with specific selectivity containing oxindole-fused spirotetrahydrofurochroman by one-pot reaction.

    abstract：:Protein tyrosine phosphatase 1B (PTP1B) has been proposed to be an ideal target for treatment of type II diabetes and obesity. However, no druggable PTP1B inhibitor has been established and there is still an urgent demand for the development of structurally novel PTPIB inhibitor. Herein, we reported core-structurally ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2016.11.055

    authors： Dong S,Lei Y,Jia S,Gao L,Li J,Zhu T,Liu S,Hu W

    更新日期：2017-02-15 00:00:00

  • Gastric-sparing nitric oxide-releasable 'true' prodrugs of aspirin and naproxen.

    abstract：:Nitric oxide-releasing non-steroidal anti-inflammatory drugs (NO-NSAIDs) are gaining attention as potentially gastric-sparing NSAIDs. Herein, we report a novel class of '1-(nitrooxy)ethyl ester' group-containing NSAIDS as efficient NO releasing 'true' prodrugs of aspirin and naproxen. While an aspirin prodrug exhibite...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2014.10.096

    authors： Gund M,Gaikwad P,Borhade N,Burhan A,Desai DC,Sharma A,Dhiman M,Patil M,Sheikh J,Thakre G,Tipparam SG,Sharma S,Nemmani KVS,Satyam A

    更新日期：2014-12-15 00:00:00

  • In vivo click reaction between Tc-99m-labeled azadibenzocyclooctyne-MAMA and 2-nitroimidazole-azide for tumor hypoxia targeting.

    abstract：:The bioactivity of nitroimidazole in Tc-99m-labeled 2-nitroimidazole, a traditional solid tumor hypoxia-imaging agent for single photon emission computed tomography (SPECT), is reduced by the presence of large ligand and metallic radionuclide, exhibiting lower tumor-to-nontumor ratios. In an effort to solve this gener...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2015.09.004

    authors： Sun W,Chu T

    更新日期：2015-10-15 00:00:00

  • N-[(3S)-Pyrrolidin-3-yl]benzamides as novel dual serotonin and noradrenaline reuptake inhibitors: impact of small structural modifications on P-gp recognition and CNS penetration.

    abstract：:The structure-activity relationship and the synthesis of novel N-[(3S)-pyrrolidin-3-yl]benzamides as dual serotonin and noradrenaline monoamine reuptake inhibitors (SNRI) is described. Preferred compound 9 aka PF-184,298 is a potent SNRI with good selectivity over dopamine reuptake inhibition (DRI), good in vitro meta...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2009.07.049

    authors： Wakenhut F,Allan GA,Fish PV,Fray MJ,Harrison AC,McCoy R,Phillips SC,Ryckmans T,Stobie A,Westbrook D,Westbrook SL,Whitlock GA

    更新日期：2009-09-01 00:00:00

  • Research on PEGylation of porcine prothrombin for improving biostability and reducing animal immunogenicity.

    abstract：:Prothrombin is a vitamin K-dependent serine protease and plays pivotal roles in both procoagulant and anticoagulant pathway of hemostasis. In this study, prothrombin purified from porcine plasma was modified through PEGylation at N-terminal residue using 40 kDa PEG-phenyl-isothiocyanate (PIT-PEG40K). The monoPEGylated...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2011.04.037

    authors： Zhou JG,Chen YM

    更新日期：2011-06-01 00:00:00

  • Carbazolothiophene-2-carboxylic acid derivatives as endothelin receptor antagonists.

    abstract：:The SmI(2)-promoted three-component coupling reaction of thiophene-2-carboxylate, indole-2-carbaldehyde and acetophenone provides an expedient route to a series of tetracyclic carbazolothiophene compounds bearing the indole and thiophene rings. Among these samples, 9-benzyl-4-methyl-4-(4-hydroxyphenyl)-10-oxo-4,10-dih...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2003.12.067

    authors： Babu G,Yu HM,Yang SM,Fang JM

    更新日期：2004-03-08 00:00:00

  • Synthesis, docking, and biological studies of phenanthrene β-diketo acids as novel HIV-1 integrase inhibitors.

    abstract：:In the present study we report the synthesis of halogen-substituted phenanthrene β-diketo acids as new HIV-1 integrase inhibitors. The target phenanthrenes were obtained using both standard thermal- and microwave-assisted synthesis. 4-(6-Chlorophenanthren-2-yl)-2,4-dioxobutanoic acid (18) was the most active compound ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2013.09.009

    authors： Sharma H,Sanchez TW,Neamati N,Detorio M,Schinazi RF,Cheng X,Buolamwini JK

    更新日期：2013-11-15 00:00:00

  • Generation of novel radiolabeled opiates through site-selective iodination.

    abstract：:Tritiated opioid radioligands have proven valuable in exploring opioid binding sites. However, tritium has many limitations. Its low specific activity and limited counting efficiency makes it difficult to examine low abundant, high affinity sites and its disposal is problematic due to the need to use organic scintilla...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2011.05.008

    authors： Majumdar S,Burgman M,Haselton N,Grinnell S,Ocampo J,Pasternak AR,Pasternak GW

    更新日期：2011-07-01 00:00:00

  • Bioisosteric modification of PETT-HIV-1 RT-inhibitors: synthesis and biological evaluation.

    abstract：:Bioisosteric substitution of the thiourea (3, 5, 7, 9) and urea (10) moiety of PETT compounds with sulfamide (1), cyanoguanidine (2, 4) and guanidine (6, 8) functionalities, and replacement of the phenethyl group with benzoylethyl group (compounds 11-20) have been studied. Synthesis and antiviral activities are descri...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(99)00675-7

    authors： Högberg M,Engelhardt P,Vrang L,Zhang H

    更新日期：2000-02-07 00:00:00

  • New monoterpene glycosides from Paeonia suffruticosa Andrews and their inhibition on NO production in LPS-induced RAW 264.7 cells.

    abstract：:Nine new monoterpene glycosides (1-9), together with 18 known compounds were obtained from the n-butanol soluble fraction of ethanol extract from Paeonia suffruticosa Andrews. Their structures were determined on the basis of chemical methods and spectroscopic data. The inhibitory effects of these compounds (except com...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2012.09.034

    authors： Ding L,Zhao F,Chen L,Jiang Z,Liu Y,Li Z,Qiu F,Yao X

    更新日期：2012-12-01 00:00:00