Selective inhibition of acetylcholinesterase in the cerebellum and hippocampus of mice following an acute treatment with malathion.

abstract：:To identify anticancer agents with high potency and low toxicity, a series of (Z)-styrylbenzene derivatives were synthesised and evaluated for anticancer activities using a panel of nine cancer cell lines and two noncancerous cell lines. Most derivatives exhibited significant anti-proliferative activities against five...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Xin YB,Li JJ,Zhang HJ,Ma J,Liu X,Gong GH,Tian YS

更新日期：2018-12-01 00:00:00

abstract：:A series of compounds incorporating 3-(3-(2/3/4-substituted phenyl)triaz-1-en-1-yl) benzenesulfonamide moieties were synthesised and their chemical structure was confirmed by physico-chemical methods. Carbonic anhydrase (CA, EC 4.2.1.1) inhibitory effects of the compounds were evaluated against human isoforms hCA I an...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Bilginer S,Gonder B,Gul HI,Kaya R,Gulcin I,Anil B,Supuran CT

更新日期：2020-12-01 00:00:00

abstract：:A new series of 6, 7-dihydroxy-3-(methylphenyl) chromenones, including three new derivatives, i.e. 6,7-dihydroxy-3-(2-methylphenyl)-2H-chromen-2-one (OPC); 6,7-dihydroxy-3-(3-methylphenyl)-2H-chromen-2-one (MPC); 6,7-dihydroxy-3-(4-methylphenyl)-2H-chromen-2-one (PPC) and one previously described, namely 6,7-dihydroxy...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Basaran I,Sinan S,Cakir U,Bulut M,Arslan O,Ozensoy O

更新日期：2008-02-01 00:00:00

abstract：:Synthesis of a novel series of structurally related pyrazoloquinoline nucleosides is described. All the newly synthesized compounds were examined for their in vitro antiviral activity against herpes simplex type-1 as shown by two different bioassays, namely; crystal violet staining or the MTS tetrazolium dye measureme...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Bekhit AA,El-Sayed OA,Aboul-Enein HY,Siddiqui YM,Al-Ahdal MN

更新日期：2004-02-01 00:00:00

abstract：:An array of novel spiro imidazolidine derivatives was synthesized in dry media and was screened for their anti-microbial activities. Structure-activity relationship results revealed that compounds 22, 23 against P.aeruginosa, 24 against S.aureus, 24, 25 against K.pneumonia, 27 against S.aureus, β-H.streptococcus, 29 a...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kanagarajan V,Thanusu J,Gopalakrishnan M

更新日期：2011-04-01 00:00:00

abstract：:The synthesis and biological evaluation of some novel thiazolofluorenones, thiazolofluorenes and thiazoloanthraquinones, substituted with amino side-chains are described. These polyheterocyclic compounds have been synthesized via the corresponding imino-1,2,3-dithiazoles. Their cytotoxic activity and their eventual se...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Chabane H,Pierre A,Leonce S,Pfeiffer B,Renard P,Thiery V,Guillaumet G,Besson T

更新日期：2004-12-01 00:00:00

abstract：:The present study shows the chemical profile and the in vitro properties (antioxidant and inhibition of nitric oxide production) of the Origanum heracleoticum L. (Lamiaceae). The ethanolic extract of the aerial parts is characterized by terpenes and fatty acids. The extract, with high total phenol and flavonoid conten...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Conforti F,Marrelli M,Menichini F,Tundis R,Statti GA,Solimene U,Menichini F

更新日期：2011-06-01 00:00:00

abstract：:Rosmarinic acid, a phytochemical compound, bears diverse pharmaceutical profile. It is composed by two building blocks: caffeic acid and a salvianic acid unit. The interaction profile, responsible for the delivery of rosmarinic acid and its two substructure components by serum albumin remains unexplored. To unveil thi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Papaemmanouil C,Chatziathanasiadou MV,Chatzigiannis C,Chontzopoulou E,Mavromoustakos T,Grdadolnik SG,Tzakos AG

更新日期：2020-12-01 00:00:00

abstract：:Drug resistance has become a major concern in the field of infection management, therefore searching for new antibacterial agents is getting more challenging. Our study presents an optimized and eco-friendly synthesis scheme for a panel of nitroalkenes bearing various functional groups in the aromatic moiety and bromi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Boguszewska-Czubara A,Lapczuk-Krygier A,Rykala K,Biernasiuk A,Wnorowski A,Popiolek L,Maziarka A,Hordyjewska A,Jasiński R

更新日期：2016-12-01 00:00:00

abstract：:A series of eighteen pyrrolo[3,2-c]pyridine derivatives were tested for inhibitory effect against FMS kinase. Compounds 1e and 1r were the most potent among all the other tested analogues (IC50 = 60 nM and 30 nM, respectively). They were 1.6 and 3.2 times, respectively, more potent than our lead compound, KIST101029 (...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： El-Gamal MI,Oh CH

更新日期：2018-12-01 00:00:00

abstract：:Tetrahydrocannabinol and other mixed cannabinoid (CB) receptors CB(1)/CB(2) receptor agonists are well established to elicit antinociceptive effects and psychomimetic actions, however, their potential for abuse have dampened enthusiasm for their therapeutic development. In an effort to refine a semi-rigid structural f...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Taher AT,Kadry HH,Allarà M,Di Marzo V,Abadi AH,Abouzid KA

更新日期：2013-06-01 00:00:00

abstract：:Quantitative structure-activity relationships (QSARs) within a series of cytochrome P450 2C9 (CYP2C9) and cytochrome P450 2C19 (CYP2C19) inhibitors are reported. In particular, it is noted that compound lipophilicity, in the form of log P values (where P is the octanol/water partition coefficient), is an important fac...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Lewis DF,Lake BG,Ito Y,Dickins M

更新日期：2006-08-01 00:00:00

abstract：:Monoacylglycerol lipase is a serine hydrolase that plays a major role in the degradation of the endocannabinoid neurotransmitter 2-arachidonoylglycerol. A wide number of MAGL inhibitors are reported in literature; however, many of them are characterised by an irreversible mechanism of action and this behavior determin...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Granchi C,Caligiuri I,Bertelli E,Poli G,Rizzolio F,Macchia M,Martinelli A,Minutolo F,Tuccinardi T

更新日期：2017-12-01 00:00:00

abstract：:Fraxamoside, a macrocyclic secoiridoid glucoside featuring a hydroxytyrosol group, was recently identified as a xanthine oxidase inhibitor (XOI) comparable in potency in vitro to the standard antigout drug allopurinol. However, this activity and its considerably higher value than its derivatives oleuropein, oleoside 1...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Vitale RM,Antenucci L,Gavagnin M,Raimo G,Amodeo P

更新日期：2017-12-01 00:00:00

abstract：:Ligand-protein docking is one of the most common techniques used in virtual screening campaigns. Despite the large number of docking software available, there is still the need of improving the efficacy of docking-based virtual screenings. To date, only very few studies evaluated the possibility of combining the resul...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Poli G,Martinelli A,Tuccinardi T

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：: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：:The activation of the β-class carbonic anhydrases (CAs, EC 4.2.1.1) from the bacteria Brucella suis and Francisella tularensis with amine and amino acids was investigated. BsuCA 1 was sensitive to activation with amino acids and amines, whereas FtuCA was not. The most effective BsuCA 1 activators were L-adrenaline and...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Angeli A,Del Prete S,Pinteala M,Maier SS,Donald WA,Simionescu BC,Capasso C,Supuran CT

更新日期：2019-12-01 00:00:00

abstract：:New hydrazone ligands (HL) derived from 5-substituted isatins and 1-(4-(2-methoxybenzyl)-6-arylpyridazin-3-yl)hydrazines and its complexes with Co(II) and Cu(II) were synthesized. The new hydrazones and their complexes were characterized by means of elemental, spectral analyses and magnetic studies. Primary cytotoxici...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kandile NG,Mohamed MI,Ismaeel HM

更新日期：2012-06-01 00:00:00

abstract：:The needs for diverse inhibitors of α-glucosidase (α-Gls) encouraged us to synthesize five different poly-hydroxy functionalized pyrimidine-fused heterocyclic (PHPFH) molecules, having either aliphatic or aromatic side chains (C1-C5) and their inhibitory activities were examined spectroscopically against yeast and mou...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Yousefi R,Alavian-Mehr MM,Mokhtari F,Panahi F,Mehraban MH,Khalafi-Nezhad A

更新日期：2013-12-01 00:00:00

abstract：:The effect of N'-nitrosonornicotine (NNN), one of the tobacco-specific nitrosamines, on the catalytic activity of glutamate dehydrogenase (GLDH) in the alpha-ketoglutarate amination, using reduced nicotinamide adenine dinucleotide as coenzyme, was studied by a chronoamperometric method. The maximum reaction rate of th...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Mao YA,Zhong KJ,Wei WZ,Wei XL,Lu HB

更新日期：2005-02-01 00:00:00

abstract：:Melatonin (N-acetyl-5-methoxytryptamine) is the chief secretory product of the pineal gland and synthesized enzymatically from serotonin (5-hydroxytryptamine). These indoleamine derivatives play an important role in the prevention of oxidative damage. In the present study, DMPD radical scavenging and cupric ion (Cu(2+...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Gulçin I

更新日期：2008-12-01 00:00:00

abstract：:Protein tyrosine phosphatase 1B (PTP1B) and α-glucosidase are important targets to treat obesity and diabetes, due to their deep correlation with insulin and leptin signalling, and glucose regulation. The methanol extract of Paulownia tomentosa fruits showed potent inhibition against both enzymes. Purification of this...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Song YH,Uddin Z,Jin YM,Li Z,Curtis-Long MJ,Kim KD,Cho JK,Park KH

更新日期：2017-12-01 00:00:00

abstract：:Recently the literature described the binding of Haptoglobin (HP) with ecotin, a fold-specific serine-proteases inhibitor with an anticoagulant profile and produced by Escherichia coli. In this work, we used some in silico and in vitro techniques to evaluate HP 3D-fold and its interaction with wild-type ecotin and two...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Sathler PC,Lourenço AL,Miceli LA,Rodrigues CR,Albuquerque MG,Cabral LM,Castro HC

更新日期：2014-04-01 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：:Novel 3(2H)-pyridazinone derivatives were designed, synthesised in satisfactory yields and evaluated in different experimental assays to assess their preliminary toxicity in vivo and anti-proliferative effects against HCT116 cell lines in vitro. Artemia salina lethality test provided LC50 values >100 µg/mL for all com...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Özdemir Z,Utku S,Mathew B,Carradori S,Orlando G,Di Simone S,Alagöz MA,Özçelik AB,Uysal M,Ferrante C

更新日期：2020-12-01 00:00:00

abstract：:A novel series of substituted pyrimidine compounds bearing N-phenylpyrazole and terminating with aryl and cyclic sulfonamido moiety were designed, synthesized, and evaluated in vitro as antiproliferative agents against a panel of 53 cell lines of different tissues at the NCI. Among them, compound 1d with p-chlorobenze...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Gamal El-Din MM,El-Gamal MI,Abdel-Maksoud MS,Yoo KH,Baek D,Choi J,Lee H,Oh CH

更新日期：2016-01-01 00:00:00

abstract：:Starting from a simple general reaction mechanism of activation of aspartic proteinases zymogens involving a uni- and a bimolecular simultaneous activation route and a reversible inhibition step, the time course equation of the zymogen, inhibitor and activated enzyme concentrations have been derived. Likewise, express...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Muñoz-López A,Sotos-Lomas A,Arribas E,Masia-Perez J,Garcia-Molina F,García-Moreno M,Varon R

更新日期：2007-04-01 00:00:00

abstract：:A new series of tertiary amine derivatives of chlorochalcone (4a∼4l) were designed, synthesized and evaluated for the effect on acetylcholinesterase (AChE) and buthylcholinesterase (BuChE). The results indicated that all compounds revealed moderate or potent inhibitory activity against AChE, and some possessed high se...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Gao XH,Zhou C,Liu HR,Liu LB,Tang JJ,Xia XH

更新日期：2017-12-01 00:00:00

abstract：:We investigated the influence of bronchodilating β2-agonists on the activity of human acetylcholinesterase (AChE) and usual, atypical and fluoride-resistant butyrylcholinesterase (BChE). We determined the inhibition potency of racemate and enantiomers of fenoterol as a resorcinol derivative, isoetharine and epinephrin...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Bosak A,Knežević A,Gazić Smilović I,Šinko G,Kovarik Z

更新日期：2017-12-01 00:00:00