当前位置： SCI文献检索 > BIOORGANIC & MEDICINAL CHEMISTRY LETTERS期刊下所有文献 > Anti-inflammatory secoiridoid glycosides from Gentianella azurea.

Anti-inflammatory secoiridoid glycosides from Gentianella azurea.

Abstract：

:A phytochemical investigation on crude extract of Gentianella azurea led to the isolation of ten new (1-10) and one known (11) secoiridoid glycosides. Their structures were unambiguously elucidated by analysis of 1D and 2D NMR. Compounds 2, 5 and 11 were found to inhibit nitric oxide (NO) production in RAW 264.7 macrophages with IC50 values of 52.78 ± 8.61, 0.69 ± 0.23 and 5.18 ± 1.33, respectively, while indomethacin, the positive control, showed an IC50 value of 1.25 ± 0.52 μM.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Huang YJ,Lu H,Yu XL,Song WB,Zhang SW,Fen LY,Xuan LJ

doi

10.1016/j.bmcl.2014.09.055

subject

Has Abstract

pub_date

2014-11-15 00:00:00

pages

5260-4

issue

22

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(14)01008-7

journal_volume

24

pub_type

杂志文章

相关文献

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS文献大全
  • Novel 12-membered non-antibiotic macrolides from erythromycin A; EM900 series as novel leads for anti-inflammatory and/or immunomodulatory agents.

    abstract：:Herein, we report the design and synthesis of the novel 12-membered non-antibiotic macrolide (8R,9S)-8,9-dihydro-6,9-epoxy-8,9-anhydropseudoerythromycin A (EM900), which was found to be a potent anti-inflammatory and/or immunomodulatory agent, capable of promoting monocyte to macrophage differentiation. This molecule ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2011.04.004

    authors： Sugawara A,Sueki A,Hirose T,Nagai K,Gouda H,Hirono S,Shima H,Akagawa KS,Omura S,Sunazuka T

    更新日期：2011-06-01 00:00:00

  • Synthesis, structure and in vitro cytostatic activity of ferrocene-Cinchona hybrids.

    abstract：:Exploring copper(I)- and ruthenium(II)-catalyzed azide-alkyne cycloadditions and a Sonogashira protocol, novel cytostatic ferrocene-cinchona hybrids were synthetized displaying significant in vitro activity on HepG-2 and HT-29 cells. Preliminary SAR studies disclosed that compounds incorporating linkers with 1,2,3-tri...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2015.12.059

    authors： Kocsis L,Szabó I,Bősze S,Jernei T,Hudecz F,Csámpai A

    更新日期：2016-02-01 00:00:00

  • An amidation/cyclization approach to the synthesis of N-hydroxyquinolinones and their biological evaluation as potential anti-plasmodial, anti-bacterial, and iron(II)-chelating agents.

    abstract：:A 26-member library of novel N-hydroxyquinolinone derivatives was synthesized by a one-pot Buchwald-type palladium catalyzed amidation and condensation sequence. The design of these rare scaffolds was inspired from N-hydroxypyridones and 2-quinolinones classes of compounds which have been shown to have rich biological...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2014.12.014

    authors： Teng Y,Suwanarusk R,Ngai MH,Srinivasan R,Ong AS,Ho B,Rénia L,Chai CL

    更新日期：2015-02-01 00:00:00

  • Novel human metabolites of the angiotensin-II antagonist tasosartan and their pharmacological effects.

    abstract：:Three novel metabolites of the angiotensin-II (A-II) receptor antagonist tasosartan have been identified in humans, and the syntheses and pharmacologic profiling of these metabolites are reported. Each metabolite bound the human A-II receptor with IC(50)s between 20 and 45nM. The in vivo effects of these compounds in ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(02)00303-7

    authors： Elokdah HM,Friedrichs GS,Chai SY,Harrison BL,Primeau J,Chlenov M,Crandall DL

    更新日期：2002-08-05 00:00:00

  • Synthesis and structure-activity relationship of N-acyl-Gly-, N-acyl-Sar- and N-blocked-boroPro inhibitors of FAP, DPP4, and POP.

    abstract：:The structure-activity relationship of various N-acyl-Gly-, N-acyl-Sar-, and N-blocked-boroPro derivatives against three prolyl peptidases was explored. Several N-acyl-Gly- and N-blocked-boroPro compounds showed low nanomolar inhibitory activity against fibroblast activation protein (FAP) and prolyl oligopeptidase (PO...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2006.11.072

    authors： Tran T,Quan C,Edosada CY,Mayeda M,Wiesmann C,Sutherlin D,Wolf BB

    更新日期：2007-03-01 00:00:00

  • A new insight on the hypochlorous acid scavenging mechanism of tryptamine and tryptophan derivatives.

    abstract：:The reaction mechanisms of hypochlorous acid (HOCl) with several tryptophan and tryptamine derivatives, previously reported to scavenge this powerful oxidant, was investigated to determine whether ionic or radical pathways were involved. For this purpose, the reaction of tryptamine and tryptophan derivatives with HOCl...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2010.09.067

    authors： Carvalho LC,Estevão MS,Ferreira LM,Fernandes E,Marques MM

    更新日期：2010-11-15 00:00:00

  • Synthesis and evaluation of novel 8-oxo-8H-cyclopenta[a]acenaphthylene-7-carbonitriles as long-wavelength fluorescent markers for hypoxic cells in solid tumor.

    abstract：:Novel bioreductive and long-wavelength fluorescent markers for hypoxic cells in solid tumor, 9-isocyano-8H-acenaphtho[l,2-b]pyrrol-8-one with the side chain of 2-nitroimidazole, were designed, synthesized, and evaluated in V79 379A Chinese hamster cells in vitro. Compounds A(2) and A(4) showed good hypoxic-oxic fluore...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2005.12.031

    authors： Liu Y,Xu Y,Qian X,Xiao Y,Liu J,Shen L,Li J,Zhang Y

    更新日期：2006-03-15 00:00:00

  • Synthesis of a Streptococcus pyogenes vaccine candidate based on the M protein PL1 epitope.

    abstract：:Group A streptococcus is a Gram-positive bacteria that causes a range of infectious diseases. Targeting the bacteria, a new self-adjuvanting vaccine candidate, incorporating a carbohydrate carrier and an amino acid-based adjuvant, was synthesised utilising carbohydrate chemistry and solid-phase peptide synthesis proce...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2008.12.013

    authors： Simerska P,Lu H,Toth I

    更新日期：2009-02-01 00:00:00

  • Heteroarylureas with fused bicyclic diamine cores as inhibitors of fatty acid amide hydrolase.

    abstract：:A series of mechanism-based heteroaryl urea fatty acid amide hydrolase (FAAH) inhibitors with fused bicyclic diamine cores is described. In contrast to compounds built around a piperazine core, most of the fused bicyclic diamine bearing analogs prepared exhibited greater potency against rFAAH than the human enzyme. Se...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2020.127463

    authors： Keith JM,Jones W,Pierce JM,Seierstad M,Palmer JA,Webb M,Karbarz M,Scott BP,Wilson SJ,Luo L,Wennerholm M,Chang L,Rizzolio M,Rynberg R,Chaplan S,Guy Breitenbucher J

    更新日期：2020-10-15 00:00:00

  • Identification of potent, nonabsorbable agonists of the calcium-sensing receptor for GI-specific administration.

    abstract：:Modulation of gastrointestinal nutrient sensing pathways provides a promising a new approach for the treatment of metabolic diseases including diabetes and obesity. The calcium-sensing receptor has been identified as a key receptor involved in mineral and amino acid nutrient sensing and thus is an attractive target fo...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2017.09.008

    authors： Sparks SM,Spearing PK,Diaz CJ,Cowan DJ,Jayawickreme C,Chen G,Rimele TJ,Generaux C,Harston LT,Roller SG

    更新日期：2017-10-15 00:00:00

  • Solid-phase synthesis of 2,3-disubstituted indoles: discovery of a novel, high-affinity, selective h5-HT2A antagonist.

    abstract：:The application of a novel solid-phase synthesis of 2,3-disubstituted indoles utilizing a carbamate indole linker is described resulting in the identification of the novel, high-affinity, selective h5-HT2A antagonist 19. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(00)00558-8

    authors： Smith AL,Stevenson GI,Lewis S,Patel S,Castro JL

    更新日期：2000-12-18 00:00:00

  • Fluorescence detection of serum albumin with a turnover-based sensor utilizing Kemp elimination reaction.

    abstract：:The Kemp elimination reaction is a well-known chemical reaction that is facilitated on a protein surface microenvironment, and in particular is highly accelerated in a unique binding pocket of serum albumin. We have designed and synthesized a fluorescently activatable coumarin derivative with a benzisoxazole scaffold ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2017.05.076

    authors： Sakamoto S,Komatsu T,Ueno T,Hanaoka K,Urano Y

    更新日期：2017-08-01 00:00:00

  • Synthesis and pharmacological evaluation of the stereoisomers of 3-carba cyclic-phosphatidic acid.

    abstract：:Cyclic phosphatidic acid (CPA) is a naturally occurring analog of lysophosphatidic acid (LPA) in which the sn-2 hydroxy group forms a five-membered ring with the sn-3 phosphate. Here, we describe the synthesis of R-3-CCPA and S-3-CCPA along with their pharmacological properties as inhibitors of lysophospholipase D/aut...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2010.09.115

    authors： Gupte R,Siddam A,Lu Y,Li W,Fujiwara Y,Panupinthu N,Pham TC,Baker DL,Parrill AL,Gotoh M,Murakami-Murofushi K,Kobayashi S,Mills GB,Tigyi G,Miller DD

    更新日期：2010-12-15 00:00:00

  • Design, syntheses, and evaluation of Taspase1 inhibitors.

    abstract：:Taspase1 is a threonine protease responsible for cleaving MLL (Mixed-Lineage Leukemia) to achieve proper HOX gene expression. Subsequent studies identified additional Taspase1 substrates including Transcription Factor IIA (TFIIA) and Drosophila HCF. Taspase1 is essential for cell proliferation and is overexpressed in ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2009.07.045

    authors： Lee JT,Chen DY,Yang Z,Ramos AD,Hsieh JJ,Bogyo M

    更新日期：2009-09-01 00:00:00

  • N-alkyl-4-piperidinyl-2,3-diarylpyrrole derivatives with heterocyclic substitutions as potent and broad spectrum anticoccidial agents.

    abstract：:Diaryl-(4-piperidinyl)-pyrrole derivatives bearing cyclic amine substituents have been synthesized and evaluated as anticoccidial agents. Improvements in potency of Et-PKG inhibition, such as azetidine derivative 3a, and broad spectrum anticoccidial activities in feed, such as morpholine derivative 8c, have been achie...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2008.01.104

    authors： Liang GB,Qian X,Feng D,Fisher M,Crumley T,Darkin-Rattray SJ,Dulski PM,Gurnett A,Leavitt PS,Liberator PA,Misura AS,Samaras S,Tamas T,Schmatz DM,Wyvratt M,Biftu T

    更新日期：2008-03-15 00:00:00

  • Bioactivity-guided identification of flavonoids with cholinesterase and β-amyloid peptide aggregation inhibitory effects from the seeds of Millettia pachycarpa.

    abstract：:Millettia pachycarpa Benth, a widely used anthelminthic drug in folk, is rich in flavonoids with various bioactivities. This study aimed to identify active flavonoids with anti-Alzheimer's disease (AD) effect from its seeds by a bioassay-guided isolation. A novel rotenoid with unusual oxidative ring-opening skeleton (...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.03.024

    authors： Tu Y,Wu C,Kang Y,Li Q,Zhu C,Li Y

    更新日期：2019-05-15 00:00:00

  • Enzymatic synthesis of monocyclic beta-lactams.

    abstract：:An Mg2+ and ATP dependent beta-lactam synthetase (BLS) catalyses formation of a beta-lactam ring during the biosynthesis of clavulanic acid, an important beta-lactamase inhibitor. An epimeric mixture of a 2-methylated derivative of the natural BLS substrate N2-(2-carboxyethyl)-L-arginine was synthesised and found to b...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(01)00806-x

    authors： Sleeman MC,MacKinnon CH,Hewitson KS,Schofield CJ

    更新日期：2002-02-25 00:00:00

  • Development of amino-pyrimidine inhibitors of c-Jun N-terminal kinase (JNK): kinase profiling guided optimization of a 1,2,3-benzotriazole lead.

    abstract：:A series of amino-pyrimidines was developed based upon an initial kinase cross-screening hit from a CDK2 program. Kinase profiling and structure-based drug design guided the optimization from the initial 1,2,3-benzotriazole hit to a potent and selective JNK inhibitor, compound 24f (JNK1 and 2 IC(50)=16 and 66 nM, resp...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2012.12.047

    authors： Palmer WS,Alam M,Arzeno HB,Chang KC,Dunn JP,Goldstein DM,Gong L,Goyal B,Hermann JC,Hogg JH,Hsieh G,Jahangir A,Janson C,Jin S,Ursula Kammlott R,Kuglstatter A,Lukacs C,Michoud C,Niu L,Reuter DC,Shao A,Silva T,Tr

    更新日期：2013-03-01 00:00:00

  • Decreasing the CYP2D6 contribution to metabolism of a CK1ε inhibitor.

    abstract：:Our internal casein kinase 1ε lead inhibitor, compound 1 was partially cleared by the polymorphic cytochrome P450 2D6. CYP2D6 involvement in metabolism implies more extensive clinical trials. We therefore wanted to reduce the contribution to clearance by this enzyme. We utilized metabolism reports for compound 1 perfo...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2018.10.031

    authors： Vaz RJ,Li Y,Metz M,Yang D,Shen H,Munson M

    更新日期：2018-12-15 00:00:00

  • Novel bis(indolyl)hydrazide-hydrazones as potent cytotoxic agents.

    abstract：:A series of bis(indolyl) hydrazide-hydrazones 5a-n were synthesized and evaluated for their cytotoxicity against selected human cancer cell lines. The reaction of indole-3-carboxaldehyde 2 with indole-3-carbohydrazide 4 in presence of catalytic amount of acetic acid afforded 5a-n in good yields. Among the synthesized ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2011.11.031

    authors： Kumar D,Maruthi Kumar N,Ghosh S,Shah K

    更新日期：2012-01-01 00:00:00

  • Discovery of TD-4306, a long-acting β2-agonist for the treatment of asthma and COPD.

    abstract：:A multivalent approach focused on amine-based secondary binding groups was applied to the discovery of long-acting inhaled β2-agonists. Addition of amine moieties to the neutral secondary binding group of an existing β2-agonist series was found to provide improved in vivo efficacy, but also led to the formation of bio...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2014.04.095

    authors： McKinnell RM,Klein U,Linsell MS,Moran EJ,Nodwell MB,Pfeiffer JW,Thomas GR,Yu C,Jacobsen JR

    更新日期：2014-07-01 00:00:00

  • Synthesis, 3D-structure and stability analyses of NRPa-308, a new promising anti-cancer agent.

    abstract：:We report herein the synthesis of a newly described anti-cancer agent, NRPa-308. This compound antagonizes Neuropilin-1, a multi-partners transmembrane receptor overexpressed in numerous tumors, and thereby validated as promising target in oncology. The preparation of NRPa-308 proved challenging because of the orthogo...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.126710

    authors： Brachet E,Dumond A,Liu WQ,Fabre M,Selkti M,Raynaud F,Hermine O,Benhida R,Belmont P,Garbay C,Lepelletier Y,Ronco C,Pagès G,Demange L

    更新日期：2019-12-15 00:00:00

  • Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity.

    abstract：:Germinal center kinase-like kinase (GLK, also known as MAP4K3) has been hypothesized to have an effect on key cellular activities, including inflammatory responses. GLK is required for activation of protein kinase C-θ (PKCθ) in T cells. Controlling the activity of T helper cell responses could be valuable for the trea...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2018.03.032

    authors： May-Dracka TL,Arduini R,Bertolotti-Ciarlet A,Bhisetti G,Brickelmaier M,Cahir-McFarland E,Enyedy I,Fontenot JD,Hesson T,Little K,Lyssikatos J,Marcotte D,McKee T,Murugan P,Patterson T,Peng H,Rushe M,Silvian L,Spilker K

    更新日期：2018-06-01 00:00:00

  • Evaluation of series of isobenzofuranone dimers as PKCalpha ligands: implication for the distance between the two ligand binding sites.

    abstract：:Protein kinase C (PKC) is a family of enzymes, which play important roles in intracellular signal transduction. To examine the distance between the two ligand binding sites (C1A and C1B) of PKC, we designed and synthesized two series of isobenzofuranone dimers. Peak binding activities were observed for the C3-acyl cha...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2004.02.098

    authors： Baba Y,Mayumi S,Hirai G,Kawasaki H,Ogoshi Y,Yanagisawa T,Hashimoto Y,Sodeoka M

    更新日期：2004-06-07 00:00:00

  • Pholasin luminescence is enhanced by addition of dehydrocoelenterazine.

    abstract：:Pholasin is a bioluminescent photoprotein of Pholas dactylus. Pholasin is a commercially available photoprotein used to measure intracellular reactive oxygen species. Although extensive efforts have been carried out to determine the chemical structure of the prosthetic (chromophore) group, it still remains unclear to ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2008.08.113

    authors： Kuse M,Tanaka E,Nishikawa T

    更新日期：2008-10-15 00:00:00

  • Design, synthesis, and structure-activity relationship studies of novel tetrazole antifungal agents with potent activity, broad antifungal spectrum and high selectivity.

    abstract：:In this letter, we report our efforts to design, synthesize and evaluate biological activities of a series of novel hybridized compounds containing 1-tetrazole and 4-pyridinyl-1,2,4-triazole-3-one. An analysis of structure-activity data indicates that the target compounds with bulky and hydrophobic side chains exhibit...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2017.12.040

    authors： Qian A,Zheng Y,Wang R,Wei J,Cui Y,Cao X,Yang Y

    更新日期：2018-02-01 00:00:00

  • Antiangiogenic properties of substituted (Z)-(±)-2-(N-benzylindol-3-ylmethylene)quinuclidin-3-ol/one analogs and their derivatives.

    abstract：:In the past half century research efforts have defined a critical role for angiogenesis in tumor growth and metastasis. We previously reported that inhibition of a novel target, ENOX1, by a (Z)-2-benzylindol-3-ylmethylene) quinuclidin-3-ol, suppressed tumor angiogenesis. The present study was undertaken in order to es...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2010.10.060

    authors： Venkateswaran A,Reddy YT,Sonar VN,Muthusamy V,Crooks PA,Freeman ML,Sekhar KR

    更新日期：2010-12-15 00:00:00

  • Structural hybridization as a facile approach to new drug candidates.

    abstract：:Structural hybridization of preclinically and clinically validated pharmacologically active molecules has emerged as a promising tool to develop new generations of safe and highly efficient drug candidates against various diseases including microbial infections, virus infections and cancer. Strategies of drug-drug com...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章,评审

    doi：10.1016/j.bmcl.2020.127514

    authors： Sampath Kumar HM,Herrmann L,Tsogoeva SB

    更新日期：2020-12-01 00:00:00

  • Structure-activity relationship of N-benzenesulfonyl matrinic acid derivatives as a novel class of coxsackievirus B3 inhibitors.

    abstract：:A novel series of N-benzenesulfonyl matrinic amine/amide and matrinic methyl ether analogues were designed, synthesized and evaluated for their in vitro anti-coxsackievirus B3 (CVB3) activities. The structure-activity relationship (SAR) studies revealed that introduction of a suitable amide substituent on position 4' ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2015.06.043

    authors： Wang SG,Kong LY,Li YH,Cheng XY,Su F,Tang S,Bi CW,Jiang JD,Li YH,Song DQ

    更新日期：2015-09-01 00:00:00

  • Modulation of multidrug resistance in tumor cells by taxinine derivatives.

    abstract：:Among a series of taxinine (1) and its designed derivatives (2-33), two taxoids (29 and 33) increased cellular accumulation of vincristine in multidrug-resistant tumor cells more potently than verapamil, while the activities of eight taxoids (11, 14-16, 22, and 30-32) were comparable with that of verapamil. These resu...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(99)00009-8

    authors： Hosoyama H,Shigemori H,Tomida A,Tsuruo T,Kobayashi J

    更新日期：1999-02-08 00:00:00