A comparative study on the effect of homobrassinolide and gibberellic acid on lipid peroxidation and antioxidant status in normal and diabetic rats.

abstract：:3-alkyl-5-aryl-1-pyrimidyl-1H-pyrazole derivatives were designed and synthesised as selective inhibitors of JNK3, a target for the treatment of neurodegenerative diseases. Following previous studies, we have designed JNK3 inhibitors to reduce the molecular weight and successfully identified a lead compound that exhibi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Oh Y,Jang M,Cho H,Yang S,Im D,Moon H,Hah JM

更新日期：2020-12-01 00:00:00

abstract：:Three series of 5-bromo-thieno[2,3-b]pyridines bearing amide or benzoyl groups at position 2 were prepared as pim-1 inhibitors. All the prepared compounds were tested for their pim-1 enzyme inhibitory activity. Two compounds (3c and 5b) showed moderate pim-1 inhibitory activity with IC50 of 35.7 and 12.71 μM, respecti...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Naguib BH,El-Nassan HB

更新日期：2016-12-01 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：:Identification of a new class of antitumor agent capable to induce apoptosis without triggering necrotic cell death event is challenging. The present communication describes the multicomponent synthesis of seven new (1S,4S)-2,5-diazabicyclo[2.2.1]heptane-dithiocarbamates and their in vitro antiproliferative activity o...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Laskar S,Sánchez-Sánchez L,López-Ortiz M,López-Muñoz H,Escobar-Sánchez ML,Sánchez AT,Regla I

更新日期：2017-12-01 00:00:00

abstract：:In an in vitro screening for human carbonic anhydrase (hCA) inhibiting agents from higher plants, the petroleum ether and ethyl acetate extracts of Magydaris pastinacea seeds selectively inhibited hCA IX and hCA XII isoforms. The phytochemical investigation of the extracts led to the isolation of ten linear furocoumar...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Fois B,Distinto S,Meleddu R,Deplano S,Maccioni E,Floris C,Rosa A,Nieddu M,Caboni P,Sissi C,Angeli A,Supuran CT,Cottiglia F

更新日期：2020-12-01 00:00:00

abstract：:The inhibitory effects of 13-epimeric estrones, D-secooxime and D-secoalcohol estrone compounds on human placental 17β-hydroxysteroid dehydrogenase type 1 isozyme (17β-HSD1) were investigated. The transformation of estrone to 17β-estradiol was studied by an in vitro radiosubstrate incubation method. 13α-Estrone inhibi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Herman BE,Szabó J,Bacsa I,Wölfling J,Schneider G,Bálint M,Hetényi C,Mernyák E,Szécsi M

更新日期：2016-01-01 00:00:00

abstract：:In this study, 14 different 2-[(1-methyl-1H-tetrazole-5-yl)thio]-1-(phenyl)ethanone derivatives (1-14) were synthesized. The structures of the obtained compounds were elucidated using IR, (1)H-NMR, (13)C-NMR and FAB(+)-MS spectral data and elemental analyses results. The compounds were screened for their anticandidal ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kaplancikli ZA,Yurttaş L,Özdemir A,Turan-Zitouni G,Işcan G,Akalın G,Abu Mohsen U

更新日期：2014-02-01 00:00:00

abstract：:The reactivity of [1,2,3]triazolo[1,5-a]pyridines 1 is described. Triazolopyridines react with electrophiles in two contrasting ways, giving 3-substituted triazolopyridines 2, or products 3, resulting from triazolo ring opening with loss of molecular nitrogen. The triazolopyridines can be lithiated at -40 degrees C by...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Abarca-González B

更新日期：2002-12-01 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：:Novel 6-substituted thiazolocarbazole derivatives have been synthesized under microwave irradiation via the corresponding imino-1,2,3-dithiazoles. In vitro antitumor potential of these polyheterocyclic compounds was evaluated. Among all the tested thiazolocarbazoles, compound 10 is the most effective in inhibiting cel...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Testard A,Picot L,Fruitier-Arnaudin I,Piot JM,Chabane H,Domon L,Thiery V,Besson T

更新日期：2004-12-01 00:00:00

abstract：:The benzimidazole derivative Schiff bases and their copper(II) (Cu(II)) mixed-polypyridyl complexes (1-4) have been synthesized and characterized by the spectral and analytical techniques. DNA binding/cleavage studies indicate a stronger binding capability for the complex 4 which is confirmed by the absorbance, viscom...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Raman N,Selvan A

更新日期：2012-06-01 00:00:00

abstract：:A series of azatricyclodiones and octahydro-benzo[f]isoindoles have been synthesized by (4+2) Diels-Alder cycloaddition of maleimides with furfuryl amine. Reaction of azatricyclodiones with isocyanates led to the respective ureides. All of the compounds were screened against a number of bacteria and fungi. One of the ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Saxena N,Singh NT,Mishra M,Keshava GB,Shukla PK,Tripathi RP

更新日期：2008-08-01 00:00:00

abstract：:This study aimed to investigate the antidiabetic, antilipidaemic and antioxidant activities of Citrus medica cv Diamante (Rutaceae) hydroalcoholic (CD) peel extract in Zucker diabetic fatty (ZDF) rats. The ability of CD to protect against oxidative stress was investigated by using different in vitro assays and in vivo...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Menichini F,Tundis R,Loizzo MR,Bonesi M,D'Angelo D,Lombardi P,Mastellone V

更新日期：2016-12-01 00:00:00

abstract：:A new series of functionalized amino acid derivatives N-substituted 1-N-(tert-butoxycarbonyl)-2,2-dimethyl-4-phenyl-5-oxazolidine carboxamide (1-17) and 1-N-substituted-3-amino-2-hydroxy-3-phenylpropane-1-carboxamide (18-34) were synthesized and evaluated for their in vitro cytotoxicity against human cancer cell lines...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kumar V,Mudgal MM,Rani N,Jha A,Jaggi M,Singh AT,Sanna VK,Singh P,Sharma PK,Irchhaiya R,Burman AC

更新日期：2009-06-01 00:00:00

abstract：:Di(2-ethylhexyl) phthalate (DEHP) is the most widely plasticizer for polyvinyl chloride (PVC) that is used in plastic tubes, in medical and paramedical devices as well as in food storage packaging. The toxicological profile of DEHP has been evaluated in a number of experimental animal models and has been extensively d...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kambia N,Renault N,Dilly S,Farce A,Dine T,Gressier B,Luyckx M,Brunet C,Chavatte P

更新日期：2008-10-01 00:00:00

abstract：:The copper(II) complexes of the type [Cu(SPF)(A(n))Cl]/[Cu(PFL)(A(n))Cl] (where SPF is sparfloxacin, PFL is pefloxacin and A(n) is 2,2'-dipyridylamine/pyridine-2-carboxalehyde/thiophene-2-carboxaldehyde) were synthesised and were found to have a pyramidal geometry with a square base. The superoxide dismutase (SOD) lik...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Patel MN,Parmar PA,Gandhi DS

更新日期：2011-04-01 00:00:00

abstract：:Chemotypes comprising the d-annulated 1,3-dihydro-2H-1-benzazepin-2-one scaffold derived from the paullone structure were found to be potent vascular endothelial growth factor receptor 2 (VEGF-R2) kinase inhibitors. Three-dimensional quantitative structure-activity relationship (3D-QSAR) and docking studies were perfo...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Lan P,Sun JR,Chen WN,Sun PH,Chen WM

更新日期：2011-06-01 00:00:00

abstract：:Usually, all newborns demonstrate high serum unconjugated bilirubin (UCB) level. UCB may induce adverse effects in the central nervous system. We aimed to evaluate the cytotoxic effects of UCB and the protective effects of docosahexaenoic acid (DHA) on astrocyte cell cultures. The viability of astrocyte cells decrease...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Becerir C,Kılıç İ,Sahin Ö,Özdemir Ö,Tokgün O,Özdemir B,Akca H

更新日期：2013-08-01 00:00:00

abstract：:The antioxidant activity of extracts from Caesalpinia sappan L. (CSL) was studied in vitro by evaluating the total phenolics, measuring the antioxidant activity by TEAC, measuring the scavenging effects on reactive oxygen species (ROS) and on reactive nitrogen species (RNS), and measuring the inhibitory effect on Cu(2...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Lee MJ,Lee HS,Kim H,Yi HS,Park SD,Moon HI,Park WH

更新日期：2010-10-01 00:00:00

abstract：CONTEXT:Tumor acidity represents a major cause of chemoresistance. Proton pump inhibitors (PPIs) can neutralize tumor acidity, sensitizing cancer cells to chemotherapy. OBJECTIVE:To compare the anti-tumor efficacy of different PPIs in vitro and in vivo. MATERIALS AND METHODS:In vitro experiments PPIs anti-tumor effic...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Lugini L,Federici C,Borghi M,Azzarito T,Marino ML,Cesolini A,Spugnini EP,Fais S

更新日期：2016-08-01 00:00:00

abstract：:Poly(ADP-ribose) polymerase (PARP)-1 inhibitor has been suggested to attenuate the ischemia-reperfusion injury. We investigated the protective effect of the cardioplegia with a PARP-1 inhibitor, 4-hydoxyquinazoline (4-HQ), against myocardial ischemia-reperfusion injury. Isolated rat hearts were perfused on a Langendor...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Yamazaki K,Tanaka S,Sakata R,Miwa S,Oriyanhan W,Takaba K,Minakata K,Marui A,Ikeda T,Toyokuni S,Komeda M,Ueda K

更新日期：2013-02-01 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：: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：: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：: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：:Twenty-five new N-[4-(benzothiazole-2-yl)phenyl]acetamide derivatives bearing different heterocyclic ring systems were synthesized using 2-(4-aminophenyl)benzothiazole structure as a pharmacophoric group. Final compounds were screened for their potential antitumor activity in vitro against approximately 60 human tumor...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Yurttaş L,Tay F,Demirayak Ş

更新日期：2015-06-01 00:00:00

abstract：:Nerve agents such as sarin, cyclosarin and tabun are organophosphorus substances able to inhibit the enzyme acetylcholinesterase (AChE; EC 3.1.1.7). AChE reactivators and anticholinergics are generally used as antidotes in the case of intoxication with these agents. None of the known AChE reactivators is able to react...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Hrabinova M,Musilek K,Jun D,Kuca K

更新日期：2006-10-01 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：:A novel series of 5-(5-nitrofuran-2-yl)-and 5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazole-2-amines bearing acyclic amine at C-2 position of thiadiazole ring were synthesized and evaluated in vitro against promastigote and amastigote forms of Leishmania major. The structure-activity of series was investigated by studying ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Tahghighi A,Emami S,Razmi S,Rezazade Marznaki F,Kabudanian Ardestani S,Dastmalchi S,Kobarfard F,Shafiee A,Foroumadi A

更新日期：2013-08-01 00:00:00

abstract：:In this study, the synthetic way to new N-pyridinyl(methyl)indolylpropanamides acting as non acidic NSAIDs has been described. Pharmacomodulation was carried out at N(1) and C(5) of the indole ring and at the level of the propanamide chain. N(3)-pyridinylmethyl-[1(4-chlorobenzyl-5-chloroindol-3-yl)propanamide represen...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Dassonville A,Lardic M,Breteche A,Nourrisson MR,Le Baut G,Grimaud N,Petit JY,Duflos M

更新日期：2008-10-01 00:00:00