Inhibition of beta-amylase activity by calcium, magnesium and zinc ions determined by spectrophotometry and isothermal titration calorimetry.

abstract：:Complexes of Mn(II), Co(II), Ni(II), Cu(II), Zn(II) and Cd(II) with the Schiff bases salicylidene-o-aminothiophenol (H2L) and thiophene-o-carboxaldeneaniline (SB) have been synthesized and characterized by elemental analyses, magnetic measurements, thermogravimetric analyses as well as infrared spectra and reflectance...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Panchal PK,Pansuriya PB,Patel MN

更新日期：2006-08-01 00:00:00

abstract：:Ranitidine is an antagonist of histamine-2 (H(2)) receptor. It is employed to treat peptic ulcer and other conditions in which gastric acidity must be reduced. Sucrase is a hydrolytic enzyme that catalyzes the breakdown of sucrose to its monomer content. A liquid of yeast sucrase was developed for treatment of congeni...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Minai-Tehrani D,Ghaffari M,Sobhani-Damavandifar Z,Minoui S,Alavi S,Osmani R,Ahmadi S

更新日期：2012-08-01 00:00:00

abstract：:Carbonic anhydrases (CAs) are widespread metalloenzymes in higher vertebrates including humans. A series of phenolic compounds, including guaiacol, 4-methylguaiacol, 4-propylguaiacol, eugenol, isoeugenol, vanillin, syringaldehyde, catechol, 3-methyl catechol, 4-methyl catechol and 3-methoxy catechol were investigated ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Scozzafava A,Passaponti M,Supuran CT,Gülçin İ

更新日期：2015-01-01 00:00:00

abstract：:The inhibition of monoamine oxidase B (MAO-B) could be an effective approach for the treatment of various neurological disorders. In this study, a series of 1, 4-benzodioxan-substituted chalcone derivatives were designed, synthesised and evaluated for their inhibitory activity against human MAO-B (hMAO-B). The majorit...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kong Z,Sun D,Jiang Y,Hu Y

更新日期：2020-12-01 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 sequence of human urotensin II (UII) has been recently established as H-Glu-Thr-Pro-Asp-Cys-Phe-Trp-Lys-Tyr-Cys-Val-OH, and it has been reported that UII is the most potent mammalian vasoconstrictor peptide identified so far. A series of UII analogues was synthesized, and the contractile activity of each compound ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Labarrère P,Chatenet D,Leprince J,Marionneau C,Loirand G,Tonon MC,Dubessy C,Scalbert E,Pfeiffer B,Renard P,Calas B,Pacaud P,Vaudry H

更新日期：2003-04-01 00:00:00

abstract：:The antioxidant properties and inhibitory effect on early tumor promoter markers of A. marmelos (25 and 50 mg/Kg b. wt. orally) have been evaluated. Male Wistar rats were pre-treated for seven consecutive days with A. marmelos prior to CCl4 (1 mL Kg(- 1) body weight p. o., in corn oil [1:1 v/v]) treatment. Pre-treatme...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Khan TH,Sultana S

更新日期：2009-04-01 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：:Dietary content of phytohormones may potentially influence metabolic processes in animal cells. This study therefore aimed to investigate the effect of two plant growth regulators homobrassinolide (HB) and gibberellic acid (GBA) on the antioxidant defense status and lipid peroxidation level in the tissues of normal an...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Muthuraman P,Srikumar K

更新日期：2009-10-01 00:00:00

abstract：:In the present study we have evaluated the antigenotoxic effects of Farnesol (FL) a 15-carbon isoprenoid alcohol against benzo (a) pyrene [B(a)P] (125 mg kg(- 1).b.wt oral) induced toxicity. B(a)P administration lead to significant induction in Cytochrome P450 (CYP) content and aryl hydrocarbon hydrolase (AHH) activit...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Jahangir T,Sultana S

更新日期：2008-12-01 00:00:00

abstract：:Analogs of pralidoxime, which is a commercial antidote for intoxication from neurotoxic organophosphorus compounds, were designed, synthesized, characterized, and tested as potential inhibitors or reactivators of acetylcholinesterase (AChE) using the Ellman's test, nuclear magnetic resonance, and molecular modeling. T...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Petronilho Eda C,Rennó Mdo N,Castro NG,da Silva FM,Pinto Ada C,Figueroa-Villar JD

更新日期：2016-12-01 00:00:00

abstract：:A large number of novel secondary sulfonamides based on the open saccharin scaffold were synthesized and evaluated as selective inhibitors of four different isoforms of human carbonic anhydrase (hCA I, II, IX and XII, EC 4.2.1.1). They were obtained by reductive ring opening of the newly synthesized N-alkylated saccha...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： D'Ascenzio M,Guglielmi P,Carradori S,Secci D,Florio R,Mollica A,Ceruso M,Akdemir A,Sobolev AP,Supuran CT

更新日期：2017-12-01 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：: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

abstract：:Carbonic anhydrases have started to emerge as new potential antibacterial targets for several pathogens. Two β-carbonic anhydrases, denominated bsCA I and bsCA II, have been isolated and characterized from the bacterial pathogen Brucella suis, the causative agent of brucellosis or Malta fever. These enzymes have been ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Köhler S,Ouahrani-Bettache S,Winum JY

更新日期：2017-12-01 00:00:00

abstract：:Previous investigations into the binding of substrates/cofactors to the PAH active site have only concentrated on Phe, thienylalanine and BH(4). This is the first reported investigation to model aliphatic thioether amino acid substrates to PAH. The clearance of the thioether substrates (4.82-79.09% of Phe) in the rat ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Patel NG,Iliadou C,Boonyapiwat B,Barlow DJ,Forbes B,Mitchell SC,Steventon GB

更新日期：2008-12-01 00:00:00

abstract：:Abstract Twenty-three phenolic compounds were isolated from Dioscorea opposita by bioactivity-guided method and their inhibitory effect against pancreatic lipase was evaluated. A total of 15 isolates reduced lipase activity at IC50 values of less than 50 µM and 3,3',5-trihydroxy-2'-methoxybibenzyl showed the highest i...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Yang MH,Chin YW,Yoon KD,Kim J

更新日期：2014-02-01 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：: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：:An extracellular thermostable alkaline serine protease enzyme from Aeribacillus pallidus C10 (GenBank No: KC333049), was purified 4.85 and 17. 32-fold with a yield of 26.9 and 19.56%, respectively, through DE52 anion exchange and Probond affinity chromatography. The molecular mass of the enzyme was determined through ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Yildirim V,Baltaci MO,Ozgencli I,Sisecioglu M,Adiguzel A,Adiguzel G

更新日期：2017-12-01 00:00:00

abstract：:Cobalt (II), copper (II), nickel (II) and zinc (II) complexes with 2-hydroxy-1-naphthaldehyde derived N-substituted sulfonamides have been synthesized and the nature of bonding and structure of compounds have been deduced from physical, analytical and spectral (IR, (1)H NMR, (13)C NMR, Mass and electronic) data. An oc...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Chohan ZH,Supuran CT

更新日期：2008-04-01 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：:QSAR analysis of a series of previously synthesised 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted-2-propanols(TDFPP) as analogues of fluconazole were tested for growth inhibitory activity against Candida albicans using computer assisted multiple regression analysis. This was in order to explore the s...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Singla RK,Bhat G V

更新日期：2010-10-01 00:00:00

abstract：:Selective PDE3 inhibitors improve cardiac contractility and may be used in congestive heart failure. However, their proarrhythmic potential is the most important side effect. In this research we designed, synthesized and evaluated the potential cardiotonic activity of thirteen PDE3 inhibitors (4-[(4-methyl-2-oxo-1,2-d...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Sadeghian H,Seyedi SM,Saberi MR,Nick RS,Hosseini A,Bakavoli M,Mansouri SM,Parsaee H

更新日期：2009-08-01 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：:The in vivo and in vitro antiandrogenic activity of four aromatic esters 10a-10d, one aliphatic ester 10e based on the pregna-4,16-diene-6, 20-dione structure and two aromatic 17c, 17d and two aliphatic valeroyloxy esters 17a, 17b based on the more saturated 4-pregnene-6,20-dione skeleton was examined. The biological ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Cabeza M,Heuze I,Sánchez M,Bratoeff E,Ramírez E,Rojas A,Orozco A,Mungía A,Agustín G,Cuatepotzo L,Gonzalez C,Palma S,Padilla D,Perez V,Jimenez G

更新日期：2005-08-01 00:00:00

abstract：:An efficient and simple microwave assisted synthesis of sulfonamide derivatives incorporating the pyridazine moiety has been developed. These sulfonamides were used for the preparation of new heterocyclic compounds via reaction with different reagents using a microwave irradiation technique. The structures of the newl...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Mohamed MI,Zaky HT,Kandile NG

更新日期：2013-12-01 00:00:00

abstract：:New, except 1d, melatonin analogue benzimidazole derivatives were synthesized and characterized in the present study. The potential role of melatonin as an antioxidant by scavenging and detoxifying ROS raised the possibility that compounds that are analogous to melatonin can also be used for their antioxidant properti...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Gurer-Orhan H,Orhan H,Suzen S,Püsküllü MO,Buyukbingol E

更新日期：2006-04-01 00:00:00

abstract：:An efficient and economical synthesis of some new fluorine substituted phthalides was accomplished from two γ-keto acids, 2-(4-fluorobenzoyl)benzoic acid and 2-(3,5-dinitro-4-flurobenzoyl)benzoic acid. Each acid was reacted with various phenolic compounds in presence of catalytic quantity of concentrated sulphuric aci...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Chamoli T,Rawat MS,Jacob M

更新日期：2012-10-01 00:00:00

abstract：:Histamine H3 receptors (H3R) antagonists/inverse agonists are becoming a promising therapeutic approach for epilepsy. In this article, novel nonimidazole H3R antagonists/inverse agonists have been designed and synthesised via hybriding the H3R pharmacophore (aliphatic amine with propyloxy chain) with the 1,2,4-triazol...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Song M,Yan R,Zhang Y,Guo D,Zhou N,Deng X

更新日期：2020-12-01 00:00:00