Acetylesterase from orange peel as biocatalyst for the chemo- and regioselective deprotection of carbohydrates.


:The enzyme acetylesterase from the flavedo of oranges (EC can advantageously be applied for the chemo- and regioselective deprotection of different types of carbohydrates. It displays a selectivity which in many cases is complementary to the application of other biocatalysts or classical chemical methods.


Bioorg Med Chem


Waldmann H,Heuser A




Has Abstract


1994-06-01 00:00:00












  • Heat shock proteins: A dual carrier-adjuvant for an anti-drug vaccine against heroin.

    abstract::Heroin is a highly abused opioid that has reached epidemic status within the United States. Yet, existing therapies to treat addiction are inadequate and frequently result into rates of high recidivism. Vaccination against heroin offers a promising alternative therapeutic option but requires further development to enh...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Hwang CS,Ellis B,Zhou B,Janda KD

    更新日期:2019-01-01 00:00:00

  • Synthesis of 3-acyloxyxanthone derivatives as α-glucosidase inhibitors: A further insight into the 3-substituents' effect.

    abstract::Considerable interest has been attracted in xanthone and its derivatives because of their important biological activities. In this paper, a series of novel 3-arylacyloxyxanthone derivatives 2a-p were synthesized and evaluated for their biological activities toward α-glucosidase. In comparison to the parent 1,3-dihydro...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Li GL,Cai CY,He JY,Rao L,Ma L,Liu Y,Wang B

    更新日期:2016-04-01 00:00:00

  • Protective effect of ε-viniferin on β-amyloid peptide aggregation investigated by electrospray ionization mass spectrometry.

    abstract::Abnormal β-amyloid peptide accumulation and aggregation is considered to be responsible for the formation and cerebral deposition of senile plaques in the brains of patients with Alzheimer's disease (AD). Inhibition of the formation of β-amyloid (Aβ) fibrils would be an attractive therapeutic target for the treatment ...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Richard T,Poupard P,Nassra M,Papastamoulis Y,Iglésias ML,Krisa S,Waffo-Teguo P,Mérillon JM,Monti JP

    更新日期:2011-05-15 00:00:00

  • New triterpenoid saponins with strong alpha-glucosidase inhibitory activity from the roots of Gypsophila oldhamiana.

    abstract::Seven new triterpenoid saponins (1-7), have been isolated and elucidated from the roots of Gypsophila oldhamiana together with five known triterpenoid saponins (8-12). These saponins which could be classified into three series: 3-O-monoglucosides (1, 8, 9), 28-O-monoglucosides (2-4, 12) and 3, 28-O-bidesmosides (5-7, ...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Luo JG,Ma L,Kong LY

    更新日期:2008-03-15 00:00:00

  • The discovery of UK-369003, a novel PDE5 inhibitor with the potential for oral bioavailability and dose-proportional pharmacokinetics.

    abstract::This paper describes our recent efforts to design and synthesise potent and selective PDE5 inhibitors and the use of in vitro predictors of clearance, absorption and permeability to maximise the potential for dose-proportional pharmacokinetics and good oral bioavailability in man. Optimisation of the preclinical profi...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Rawson DJ,Ballard S,Barber C,Barker L,Beaumont K,Bunnage M,Cole S,Corless M,Denton S,Ellis D,Floc'h M,Foster L,Gosset J,Holmwood F,Lane C,Leahy D,Mathias J,Maw G,Million W,Poinsard C,Price J,Russel R,Street S

    更新日期:2012-01-01 00:00:00

  • Design, synthesis and evaluation of flurbiprofen-clioquinol hybrids as multitarget-directed ligands against Alzheimer's disease.

    abstract::A series of novel flurbiprofen-clioquinol hybrids were designed and synthesized as multifunctional agents for Alzheimer's disease therapy, and their potential was evaluated through various biological experiments. In vitro studies showed that most target compounds exhibited significant ability to inhibit self- and Cu2+...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Yang Z,Song Q,Cao Z,Yu G,Liu Z,Tan Z,Deng Y

    更新日期:2020-04-01 00:00:00

  • Synthesis and photodynamic activity of zinc(II) phthalocyanine derivatives bearing methoxy and trifluoromethylbenzyloxy substituents in homogeneous and biological media.

    abstract::Two zinc(II) phthalocyanines bearing either four methoxy (ZnPc 3) or trifluoromethylbenzyloxy (ZnPc 4) substituents have been synthesized by a two-step procedure starting from 4-nitrophthalonitrile. Absorption and fluorescence spectroscopic studies were analyzed in different media. These compounds are essentially non-...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Yslas EI,Rivarola V,Durantini EN

    更新日期:2005-01-03 00:00:00

  • Inhibition of secreted phospholipases A₂ by 2-oxoamides based on α-amino acids: Synthesis, in vitro evaluation and molecular docking calculations.

    abstract::Group IIA secreted phospholipase A₂ (GIIA sPLA₂) is a member of the mammalian sPLA₂ enzyme family and is associated with various inflammatory conditions. In this study, the synthesis of 2-oxoamides based on α-amino acids and the in vitro evaluation against three secreted sPLA₂s (GIIA, GV and GX) are described. The lon...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Mouchlis VD,Magrioti V,Barbayianni E,Cermak N,Oslund RC,Mavromoustakos TM,Gelb MH,Kokotos G

    更新日期:2011-01-15 00:00:00

  • Fluoroalkene modification of mercaptoacetamide-based histone deacetylase inhibitors.

    abstract::Inhibitors of histone deacetylases (HDAC) are emerging as a promising class of anti-cancer agents. The mercaptoacetoamide-based inhibitors are reported to be less toxic than hydroxamate and are worthy of further consideration. Therefore, we have designed a series of analogs as potential inhibitors of HDACs, in which t...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Osada S,Sano S,Ueyama M,Chuman Y,Kodama H,Sakaguchi K

    更新日期:2010-01-15 00:00:00

  • 1,2,3-Triazolyl-4-oxoquinolines: A feasible beginning for promising chemical structures to inhibit oseltamivir-resistant influenza A and B viruses.

    abstract::We described the synthesis of a new congener series of 1,2,3-triazolyl-4-oxoquinolines and evaluated their ability to inhibit oseltamivir (OST)-resistant influenza strains. Oxoquinoline derivative 1i was the most potent compound within this series, inhibiting 94% of wild-type (WT) influenza neuraminidase (NA) activity...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Boechat Fda C,Sacramento CQ,Cunha AC,Sagrillo FS,Nogueira CM,Fintelman-Rodrigues N,Santos-Filho O,Riscado CS,Forezi Lda S,Faro LV,Brozeguini L,Marques IP,Ferreira VF,Souza TM,de Souza MC

    更新日期:2015-12-15 00:00:00

  • Structure-activity relationships in platelet-activating factor. Part 14: synthesis and biological evaluation of piperazine derivatives with dual anti-PAF and anti-HIV-1 activity.

    abstract::As HIV-associated dementia prevalence has risen with the lifespan of HIV-infected individuals, there is an important need for antiretroviral and anti-inflammatory drugs targeting the central nervous system. Platelet-activating factor, a mediator of inflammation, is an HIV-induced neurotoxin secreted in the infected br...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Sallem W,Serradji N,Dereuddre-Bosquet N,Dive G,Clayette P,Heymans F

    更新日期:2006-12-01 00:00:00

  • Branched-chain and unsaturated 1,7-diaminoheptane derivatives as deoxyhypusine synthase inhibitors.

    abstract::Deoxyhypusine synthase catalyzes the first step in the posttranslational biosynthesis of the unusual amino acid hypusine [N epsilon-(4-amino-2-hydroxybutyl)lysine] in eukaryotic translation initiation factor 5A (eIF-5A). eIF-5A and its single hypusine residue are essential for cell proliferation. Two series of 1,7-dia...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Lee YB,Folk JE

    更新日期:1998-03-01 00:00:00

  • Novel 4-acetamide-2-alkylthio-N-acetanilides resembling nimesulide: Synthesis, cell viability evaluation and in silico studies.

    abstract::Since nimesulide, a nonsteroidal anti-inflammatory drug, is known to be a selective inhibitor of cyclooxygenase-2 and shows activity against cancer cells, there has been much interest in developing related molecules with enhanced anticancer properties. Taking in consideration structural features of nimesulide analogue...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Catarro M,Serrano J,Cavalheiro E,Ramos S,Santos AO,Silvestre S,Almeida P

    更新日期:2017-08-15 00:00:00

  • Transdermal penetration behaviour of drugs: CART-clustering, QSPR and selection of model compounds.

    abstract::A set of 116 structurally very diverse compounds, mainly drugs, was characterized by 1630 molecular descriptors. The biological property modelled in this study was the transdermal permeability coefficient logK(p). The main objective was to find a limited set of suitable model compounds for skin penetration studies. Th...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Baert B,Deconinck E,Van Gele M,Slodicka M,Stoppie P,Bodé S,Slegers G,Vander Heyden Y,Lambert J,Beetens J,De Spiegeleer B

    更新日期:2007-11-15 00:00:00

  • Design, synthesis, conformational analysis, and biological studies of urotensin-II lactam analogues.

    abstract::Human urotensin II (hU-II; H-Glu-Thr-Pro-Asp-cyclo[Cys-Phe-Trp-Lys-Tyr-Cys]-Val-OH) is a disulfide bridged undecapeptide recently identified as the ligand of an orphan G protein-coupled receptor. hU-II has been described as the most potent vasoconstrictor compound identified to date. With the aim of replacing the disu...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Grieco P,Carotenuto A,Patacchini R,Maggi CA,Novellino E,Rovero P

    更新日期:2002-12-01 00:00:00

  • Structure-activity study of epi-gallocatechin gallate (EGCG) analogs as proteasome inhibitors.

    abstract::The structure-activity relationship of a number of synthetic green tea polyphenol analogs involving modifications of A ring and B ring of epi-gallocatechin gallate (EGCG) as proteasome inhibitors has been examined. It was found that in B ring, a decrease in the number of OH groups led to decreased potency. Introductio...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Wan SB,Landis-Piwowar KR,Kuhn DJ,Chen D,Dou QP,Chan TH

    更新日期:2005-03-15 00:00:00

  • Inhibition of thioredoxin reductase by a novel series of bis-1,2-benzisoselenazol-3(2H)-ones: Organoselenium compounds for cancer therapy.

    abstract::Thioredoxin reductase (TrxR) is critical for cellular redox regulation and is involved in tumor proliferation, apoptosis and metastasis. Its C-terminal redox-active center contains a cysteine (Cys497) and a unique selenocysteine (Sec498), which are exposed to solvent and easily accessible. Thus, it is becoming an impo...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: He J,Li D,Xiong K,Ge Y,Jin H,Zhang G,Hong M,Tian Y,Yin J,Zeng H

    更新日期:2012-06-15 00:00:00

  • Solid-phase synthesis of a combinatorial library of dihydroceramide analogues and its activity in human alveolar epithelial cells.

    abstract::Solid-phase synthesis of a small combinatorial library of dihydroceramide analogues as mixtures of erythro and threo diastereomers is described. Some dihydroceramide analogues cause growth arrest and apoptosis in a dose-dependent manner in human alveolar epithelial cells. This activity is likely due to the threo isome...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Villorbina G,Canals D,Carde L,Grijalvo S,Pascual R,Rabal O,Teixidó J,Fabriàs G,Llebaria A,Casas J,Delgado A

    更新日期:2007-01-01 00:00:00

  • Synthesis and structure-activity correlations of the cytotoxic bifunctional 1,4-diamidoanthraquinone derivatives.

    abstract::Anthraquinone-based compounds are attractive target for the design of new anticancer drugs. We have previously described a series of 1,5- and 1,4-difunctionalized anthraquinones, which exhibit different spectra of potency, together with human telomerase evaluation. The present study details the preparation of further,...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Huang HS,Chiu HF,Lee AL,Guo CL,Yuan CL

    更新日期:2004-12-01 00:00:00

  • Carbon-carbon-linked (pyrazolylphenyl)oxazolidinones with antibacterial activity against multiple drug resistant gram-positive and fastidious gram-negative bacteria.

    abstract::In an effort to expand the spectrum of activity of the oxazolidinone class of antibacterial agents to include Gram-negative bacteria, a series of new carbon-carbon linked pyrazolylphenyl analogues has been prepared. The alpha-N-substituted methyl pyrazole (10alpha) in the C3-linked series exhibited very good Gram-posi...

    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

  • Conformationally locked thiosugars as potent alpha-mannosidase inhibitors: synthesis, biochemical and docking studies.

    abstract::A series of thiosugar derivatives (thiolevomannosans) derived from mannose were synthesized and their inhibitory activity was tested against alpha-mannosidase (jack bean). These inhibitors were found to be more potent than the well-known inhibitors like kifunensine and deoxymannojirimycin based on docking and biochemi...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Sivapriya K,Hariharaputran S,Suhas VL,Chandra N,Chandrasekaran S

    更新日期:2007-09-01 00:00:00

  • ortho-Halogen naphthaleins as specific inhibitors of Lactobacillus casei thymidylate synthase. Conformational properties and biological activity.

    abstract::Thymidylate synthase (TS) (EC, an enzyme involved in the DNA synthesis of both prokaryotic and eukaryotic cells, is a potential target for the development of anticancer and antinfective agents. Recently, we described a series of phthalein and naphthalein derivatives as TS inhibitors. These compounds have str...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Ghelli S,Rinaldi M,Barlocco D,Gelain A,Pecorari P,Tondi D,Rastelli G,Costi MP

    更新日期:2003-03-20 00:00:00

  • Synthesis and evaluation of water-soluble docetaxel prodrugs-docetaxel esters of malic acid.

    abstract::The synthesis of docetaxel esters of malic acid is described. These compounds were found to have greatly improved water solubility and are stable in solution at neutral pH. The C2' modified compounds 2a-c and 3a-c behave as prodrugs, that is, docetaxel is generated upon exposure to human plasma, whereas the C7 and C2'...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Du W,Hong L,Yao T,Yang X,He Q,Yang B,Hu Y

    更新日期:2007-09-15 00:00:00

  • Flavonoids as noncompetitive inhibitors of Dengue virus NS2B-NS3 protease: inhibition kinetics and docking studies.

    abstract::NS2B-NS3 is a serine protease of the Dengue virus considered a key target in the search for new antiviral drugs. In this study flavonoids were found to be inhibitors of NS2B-NS3 proteases of the Dengue virus serotypes 2 and 3 with IC50 values ranging from 15 to 44 μM. Agathisflavone (1) and myricetin (4) turned out to...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: de Sousa LR,Wu H,Nebo L,Fernandes JB,da Silva MF,Kiefer W,Kanitz M,Bodem J,Diederich WE,Schirmeister T,Vieira PC

    更新日期:2015-02-01 00:00:00

  • Inhibitory activity of a ceramide library on interleukin-4 production from activated T cells.

    abstract::Allergic diseases are hypersensitivity disorders associated with the production of specific immunoglobulin E (IgE) to environmental allergens. Interleukin (IL)-4, produced primarily by CD4(+) T cells, is an important stimulus for the switch of the antibody isotype to IgE in both mice and humans. In this study we inves...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Park J,Li Q,Chang YT,Kim TS

    更新日期:2005-04-01 00:00:00

  • Properties of diacetyl (acetoin) reductase from Bacillus stearothermophilus.

    abstract::The cells of Bacillus stearothermophilus contain an NADH-dependent diacetyl (acetoin) reductase. The enzyme was easily purified to homogeneity, partially characterised, and found to be composed of two subunits with the same molecular weight. In the presence of NADH, it catalyses the stereospecific reduction of diacety...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Giovannini PP,Medici A,Bergamini CM,Rippa M

    更新日期:1996-08-01 00:00:00

  • Inhibition studies of the β-carbonic anhydrases from the bacterial pathogen Salmonella enterica serovar Typhimurium with sulfonamides and sulfamates.

    abstract::The two β-carbonic anhydrases (CAs, EC from the bacterial pathogen Salmonella enterica serovar Typhimurium, stCA 1 and stCA 2, were investigated for their inhibition with a large panel of sulfonamides and sulfamates. Unlike inorganic anions, which are weak, millimolar inhibitors of the two enzymes [Vullo et a...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Nishimori I,Minakuchi T,Vullo D,Scozzafava A,Supuran CT

    更新日期:2011-08-15 00:00:00

  • Structural study of four-stranded quadruplex structures containing 2'-deoxy-8-(propyn-1-yl)adenosine.

    abstract::In this paper, we report the NMR structural study of two quadruplex structures formed by truncations of the human telomeric sequence and containing a modified base, namely d(AprGGGT) and d(TAprGGGT), where Apr indicates 2'-deoxy-8-(propyn-1-yl)adenosines. Both oligonucleotides have been found to form 4-fold symmetric ...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Esposito V,Randazzo A,Galeone A,Varra M,Mayol L

    更新日期:2004-03-01 00:00:00

  • Spirooxindole-pyrrolidine heterocyclic hybrids promotes apoptosis through activation of caspase-3.

    abstract::A small library of spirooxindole-pyrrolidine hybrids have been synthesized for the first time in an ionic liquid, [bmim]Br in good to excellent yields employing a new class of non-stabilized azomethine ylides derived from isatin and tyrosine, a combination that has been rarely employed for the in situ generation of az...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Kumar RS,Almansour AI,Arumugam N,Mohammad F,Kotresha D,Menéndez JC

    更新日期:2019-06-15 00:00:00

  • Enediyne-mediated cleavage of RNA.

    abstract::RNA cleavage by enediyne anticancer antibiotics was shown to occur with no apparent sequence selectivity, but RNA structure appears to be important in those substrates where cleavage was observed. Neocarzinostatin (NCS) cleaved a wider variety of RNA substrates than either esperamicin (ESP) or calicheamicin (CAL), and...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Battigello JM,Cui M,Roshong S,Carter BJ

    更新日期:1995-06-01 00:00:00