Biochemical characterisation of a Kunitz-type inhibitor from Tamarindus indica L. seeds and its efficacy in reducing plasma leptin in an experimental model of obesity.

abstract：:Seven triterpenoid saponins were identified in methanolic extracts of seeds of the Zolfino bean landrace (Phaseolus vulgaris L.) by HPLC fractionation, revealing their ability to inhibit highly purified human recombinant aldose reductase (hAKR1B1). Six of these compounds were associated by MS analysis with the followi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Balestri F,De Leo M,Sorce C,Cappiello M,Quattrini L,Moschini R,Pineschi C,Braca A,La Motta C,Da Settimo F,Del-Corso A,Mura U

更新日期：2019-12-01 00:00:00

abstract：:A series of N1-(substituted)aryl-5,7-dimethyl-2-(substituted)pyrido(2,3-d)pyrimidin-4(3H)-one was designed on the basis of the triangular pharmacophoric requirement of histamine H1-receptor antagonists. The designed series was synthesized by cyclo-condensation of monoaryl thiourea with ethyl cyanoacetate in the presen...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Suhagia BN,Chhabria MT,Makwana AG

更新日期：2006-12-01 00:00:00

abstract：:Enzyme inhibition by fullerene derivatives has attracted much attention. In this communication, effects of two water-solube fullerene derivatives, fullerol and trimalonic acid C60 (TMA C60) on polymerase chain reaction (PCR) were investigated by using PCR of beta-actin cDNA derived from HeLa cells as an experimental m...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Meng X,Li B,Chen Z,Yao L,Zhao D,Yang X,He M,Yu Q

更新日期：2007-06-01 00:00:00

abstract：:Coumarin, a naturally occurring or synthesised phytochemical, displays a wide range of biological activities. However, chromen-2-ones fused with 1,3-benzoxazine rings is not well documented and there is a gap in the literature which required engaging. The substituted-2-thioxo-chromen-oxazine linear compounds 14a-i and...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Morrison R,Al-Rawi JM

更新日期：2016-01-01 00:00:00

abstract：:A series of N-(5-methyl-isoxazol-3-yl/1,3,4-thiadiazol-2-yl)-4-(3-substitutedphenylureido) benzenesulfonamide derivatives has been designed, synthesized and screened for their in vitro human carbonic anhydrase (hCA; EC 4.2.1.1) inhibition potential. These newly synthesized sulfonamide compounds were assessed against i...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Mishra CB,Kumari S,Angeli A,Monti SM,Buonanno M,Prakash A,Tiwari M,Supuran CT

更新日期：2016-01-01 00:00:00

abstract：:Cytosine deaminase (CD) from Aspergillus parasiticus, which has half-life of 1.10 h at 37°C, was stabilized by immobilization on calcium alginate beads. The immobilized CD had pH and temperature optimum of 5 and 50°C respectively. The immobilized enzyme also stoichiometrically deaminated Cytosine and 5-fluorocytosine ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Zanna H,Nok AJ,Ibrahim S,Inuwa HM

更新日期：2013-12-01 00:00:00

abstract：:In the present study, a new series of 2-[4-(pyrimidin-2-yl)piperazin-1-yl]-2-oxoethyl 4-substituted piperazine-1-carbodithioate derivatives (2a-n) were synthesized and screened for their monoamine oxidase A and B inhibitory activity. The structures of compounds were elucidated using spectroscopic methods and some phys...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kaya B,Yurttaş L,Sağlik BN,Levent S,Özkay Y,Kaplancikli ZA

更新日期：2017-12-01 00:00:00

abstract：:The galangal (the rhizome of Alpinia officinarum, Hance) is popular in Asia as a traditional herbal medicine. The present study reports that the galangal extract (GE) can potently inhibit fatty-acid synthase (FAS, E.C.2.3.1.85). The inhibition consists of both reversible inhibition with an IC50 value of 1.73 microg dr...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Li BH,Tian WX

更新日期：2003-08-01 00:00:00

abstract：:Initial velocity enzyme kinetics was used to study the inhibition mechanism of guanidine hydrochloride (Gdm.Cl) on catalytic activity of recombinant human protein disulfide isomerase (rhPDI) in protein folding. Reduced C125A recombinant human interleukin 2 (C125A rhIL-2), the substrate, was dissolved in 8 M Gdm.Cl bef...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Du C,Wolfe JL

更新日期：2003-02-01 00:00:00

abstract：:A new series of compounds derived from thiophene-2-carboxamide were synthesized and characterized by IR, (1)H-NMR and (13)C-NMR, mass spectrometry and elemental analysis. These compounds were further used to prepare their Co(II), Ni(II), Cu(II) and Zn(II) metal complexes. All metal(II) complexes were air and moisture ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Sumrra SH,Hanif M,Chohan ZH,Akram MS,Akhtar J,Al-Shehri SM

更新日期：2016-08-01 00:00:00

abstract：:Phytochemical investigations on the n-BuOH-soluble fraction of the whole plant of Buddleja davidii led to the isolation of the phenylpropanoid glycosides 1-10. Their structures were determined by 1D and 2D NMR spectroscopic techniques. All the compounds showed potent antioxidative activity in three different tests, wi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ahmad I,Ahmad N,Wang F

更新日期：2009-08-01 00:00:00

abstract：:Nineteen 5-nitrothiazolylthiosemicarbazones were synthesized from 5-nitrothiazole by three-step synthesis and evaluated for in vitro activities against seven mycobacterial species. Among them, N-(5-nitro-1, 3-thiazol-2-yl)-2-((Z)-4-[(phenylmethyl)oxy]phenylmethylidene)hydrazine-1-carbothioamide (4m) was found to be th...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Sriram D,Yogeeswari P,Senthilkumar P,Sangaraju D

更新日期：2010-02-01 00:00:00

abstract：:The synthesis of 2-isopropenyl-2,3-dihydrobenzofuranic enantioisomers is described. Ortho-(2-hydroxy-3-methyl-but-3-enyl)phenol synthons are used as precursors to these structures. In vitro antitumor activity against a non-small-cell bronchopulmonary carcinoma line (NSCLC-N6) of these enantioisomers has been investiga...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Hélesbeux JJ,Duval O,Séraphin D,Roussakis C,Richomme P

更新日期：2003-04-01 00:00:00

abstract：:The inhibitory effect of four structurally related flavonoids, apigenin, baicalein, luteolin and quercetin on the matrix metalloproteinase (MMP)-9 and -13 expressions in osteoblasts was investigated. Treatment with IL-1β induced both MMP-9 and -13 mRNA expressions as measured by quantitative real-time PCR. Luteolin an...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Yang H,Liu Q,Ahn JH,Kim SB,Kim YC,Sung SH,Hwang BY,Lee MK

更新日期：2012-04-01 00:00:00

abstract：:During the treatment of tuberculosis infection, oxidative stress due to anti-tubercular drugs may result in tissue inflammation. It was suggested that treatment with antioxidant drugs could be beneficial as an adjunct to anti-tuberculosis drug therapy. Recently our group has shown that several C-glycosides are inhibit...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Zaro MJ,Bortolotti A,Riafrecha LE,Concellón A,Morbidoni HR,Colinas PA

更新日期：2016-12-01 00:00:00

abstract：:Numerous studies have highlighted the implications of the glycogen synthase kinase 3 (GSK-3) in several processes associated with Alzheimer's disease (AD). Therefore, GSK-3 has become a crucial therapeutic target for the treatment of this neurodegenerative disorder. Hereby, we report the design and multistep synthesis...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Sciú ML,Sebastián-Pérez V,Martinez-Gonzalez L,Benitez R,Perez DI,Pérez C,Campillo NE,Martinez A,Moyano EL

更新日期：2019-12-01 00:00:00

abstract：CONTEXT:Endocrinological factors have been recently described to affect respiratory mechanics. OBJECTIVE:To review recent literature data, most of all obtained by the end-inflation occlusion method, describing the effects of molecules of endocrinological interest such as endothelin, erythropoietin and renin-angiotensi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Rubini A,Frigo A,Carniel EL

更新日期：2016-12-01 00:00:00

abstract：:Adult male ICR mice were treated by intraperitoneal injection with 250 mg/kg of bodyweight of commercial malathion (a dose corresponding to 1/12 the LD50). After 6 h, acetylcholinesterase (AChE) activity in blood, liver, and six brain regions was determined. A statistically significant inhibition was observed in whole...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Banasik M,Stedeford T,Persad AS,Ueda K,Tanaka S,Muro-Cacho C,Harbison RD

更新日期：2003-12-01 00:00:00

abstract：UNLABELLED:Abstract In biological systems, the Keap1/Nrf2/antioxidant response element pathway determines the ability of mammalian cells to adapt and survive conditions of oxidative, electrophilic and inflammatory stress by regulating the production of cytoprotective enzymes NAD(P)H:quinone oxidoreductase 1 (NQO1, EC ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ghorab MM,Higgins M,Alsaid MS,Arafa RK,Shahat AA,Dinkova-Kostova AT

更新日期：2014-12-01 00:00:00

abstract：:The design of multi-target directed ligands (MTDLs) is a valid approach for obtaining effective drugs for complex pathologies. MTDLs that combine neuro-repair properties and block the first steps of neurotoxic cascades could be the so long wanted remedies to treat neurodegenerative diseases (NDs). By linking two privi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Estrada-Valencia M,Herrera-Arozamena C,Pérez C,Viña D,Morales-García JA,Pérez-Castillo A,Ramos E,Romero A,Laurini E,Pricl S,Rodríguez-Franco MI

更新日期：2019-12-01 00:00:00

abstract：:Previously, a glycoglycerolipid isolated from marine algae was reported to be a potent and selective inhibitor of the human Myt1 kinase, an enzyme involved in cell cycle regulation with great potential as an anti-cancer target. Based on that report, a lot of research effort has been invested by several working groups ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Rohe A,Göllner C,Erdmann F,Sippl W,Schmidt M

更新日期：2015-06-01 00:00:00

abstract：:Corticosteroids are anti-inflammatory drugs that are similar to the natural corticosteroid hormones produced by the cortex of the adrenal glands. The objective of this study was to scrutinize effects of some corticosteroids on glucose-6-phosphate dehydrogenase (G6PD) and some antioxidant enzymes. Initially, G6PD was p...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ozmen I

更新日期：2005-02-01 00:00:00

abstract：:Inflammatory bowel disease (IBD) is a chronic immuno-inflammation in gastrointestinal tract. We have evaluated the activity of the compounds to inhibit the adhesion of monocytes to colon epithelial cells is triggered by a pro-inflammatory cytokine, tumour necrosis factor (TNF)-α. The in vitro activity of the compounds...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Chaudhary CL,Gurung P,Jang S,Banskota S,Nam TG,Kim JA,Jeong BS

更新日期：2020-12-01 00:00:00

abstract：:Structural modifications around 8-HETE (8-hydroxyeicosatetraenoic acid), a natural agonist of the PPAR (peroxisome proliferator-activated receptor) nuclear receptors have led previously to the identification of a promising analog, the quinoline S 70655. Series of novel quinoline or benzoquinoline derivatives were desi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Liutkus M,Caijo F,Girard AL,Ayral E,Audinot V,Boutin JA,Renard P,Caignard DH,Dacquet C,Ktorza A,Mosset P,Grée R

更新日期：2010-10-01 00:00:00

abstract：:The increasing clinical importance of drug-resistant mycobacterial pathogens has lent additional urgency to microbiological research and new antimycobacterial compound development. For this purpose, new triazoles were synthesized and evaluated for antituberculosis activity. A series of 4-arylidenamino-4H-1,2,4-triazol...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ozdemir A,Turan-Zitouni G,Kaplancikli ZA,Chevallet P

更新日期：2007-08-01 00:00:00

abstract：:The trypanocidal activity of N-allyl (NAOx) and N-propyl (NPOx) oxamates and that of the ethyl esters ofN-allyl (Et-NAOx) and N-propyl (Et-NPOx) oxamates were tested on cultured epimastigotes (in vitro) and murine trypanosomiasis (in vivo) using five different T. cruzi strains. NAOx and NPOx did not penetrate intact e...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Aguirre-Alvarado C,Zaragoza-Martínez F,Rodríguez-Páez L,Nogueda B,Baeza I,Wong C

更新日期：2007-04-01 00:00:00

abstract：:A small library of phosphorylated sulfamates (N-(O-alkylsulfamoyl)-phosphoramidic acids) incorporating long aliphatic chains (C8-C16) has been synthesized and investigated for their interaction with two physiologically relevant carbonic anhydrase (CA) isozymes. These compounds behaved as very potent inhibitors of both...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Bonnac L,Innocenti A,Winum JY,Casini A,Montero JL,Scozzafava A,Barragan V,Supuran CT

更新日期：2004-06-01 00:00:00

abstract：:In this study, firstly, antioxidant and polyphenol oxidase (PPO) properties of Yomra apple were investigated. Seventeen phenolic constituents were measured by reverse phase-high-performance liquid chromatography (RP-HPLC). Total phenolic compounds (TPCs), ferric reducing antioxidant power (FRAP) and 2, 2-diphenyl-1-pi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Can Z,Dincer B,Sahin H,Baltas N,Yildiz O,Kolayli S

更新日期：2014-12-01 00:00:00

abstract：:The hypoxic tumour microenvironment of solid tumours represents an important starting point for modulating progression and metastatic spread. Carbonic anhydrase IX (CAIX) is a known HIF-1α-dependent key player in maintaining cell pH conditions under hypoxia. We show that CAIX is strongly expressed in esophageal carcin...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Drenckhan A,Freytag M,Supuran CT,Sauter G,Izbicki JR,Gros SJ

更新日期：2018-12-01 00:00:00

abstract：:Reaction of thiophosgene with 4-aminomethyl-benzenesulfonamide afforded 4-isothiocyanatomethyl-benzenesulfonamide, which by reaction with amines, amino acids and oligopeptides, lead to a series of new sulfonamides incorporating a 4-sulfamoylphenylmethylthiourea scaffold. These new thioureas showed strong affinities to...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Casini A,Scozzafava A,Mincione F,Menabuoni L,Supuran CT

更新日期：2002-10-01 00:00:00