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：: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

abstract：:Photodynamic molecules represent an alternative approach for cancer therapy for their property (i) to be photo-reactive; (ii) to be not-toxic for target cells in absence of light; (iii) to accumulate specifically into tumour tissues; (iv) to be activable by a light beam only at the tumour site and (v) to exert cytotox...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kusuzaki K,Matsubara T,Murata H,Logozzi M,Iessi E,Di Raimo R,Carta F,Supuran CT,Fais S

更新日期：2017-12-01 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：: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：: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：: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：:Human neutrophil elastase (HNE) is an important target for the development of novel and selective inhibitors to treat inflammatory diseases, especially pulmonary pathologies. Here, we report the synthesis, structure-activity relationship analysis, and biological evaluation of a new series of HNE inhibitors with an iso...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Vergelli C,Schepetkin IA,Crocetti L,Iacovone A,Giovannoni MP,Guerrini G,Khlebnikov AI,Ciattini S,Ciciani G,Quinn MT

更新日期：2017-12-01 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：:New coumaryl-carboxamide derivatives with the thiourea moiety as a linker between the alkyl chains and/or the heterocycle nucleus were synthesized and their inhibitory activity against the human carbonic anhydrase (hCA) isoforms hCA I, II, VII and IX were evaluated. While the hCA I, II and VII isoforms were not inhibi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Zengin Kurt B,Sonmez F,Durdagi S,Aksoydan B,Ekhteiari Salmas R,Angeli A,Kucukislamoglu M,Supuran CT

更新日期：2017-12-01 00:00:00

abstract：:The current study was designed to assess the inhibitory activity of Broussonetia papyrifera-derived polyphenols against 3-chymotrypsin-like and papain-like coronavirus cysteine proteases. The isolated compounds were broussochalcone B (1), broussochalcone A (2), 4-hydroxyisolonchocarpin (3), papyriflavonol A (4), 3'-(3...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Park JY,Yuk HJ,Ryu HW,Lim SH,Kim KS,Park KH,Ryu YB,Lee WS

更新日期：2017-12-01 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：: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：: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：: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：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：:3,6-Diazaphenothiazines were obtained in cyclization of 3-amino-3'-nitro-2,4'-dipyridinyl sulfide and the reaction of sodium 3-amino-2-pyridinethiolate with 4-chloro-3-nitropyridine followed by alkylation and heteroarylation. The thiazine ring formation ran via the Smiles rearrangement. The structure elucidation was b...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Morak-Młodawska B,Pluta K,Latocha M,Suwińska K,Jeleń M,Kuśmierz D

更新日期：2016-12-01 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：:A series of hydroxylic compounds (1-10, NK-154 and NK-168) have been assayed for the inhibition of three physiologically relevant carbonic anhydrase isozymes, the cytosolic isozymes I, II and tumor-associated isozyme IX. The investigated compounds showed inhibition constants in the range of 0.068-4003, 0.012-9.9 and 0...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Durdagi S,Korkmaz N,Işık S,Vullo D,Astley D,Ekinci D,Salmas RE,Senturk M,Supuran CT

更新日期：2016-12-01 00:00:00

abstract：:Thirty new aryl-pyridazinone-substituted benzenesulphonylurea derivatives (I-XXX) were synthesized and evaluated for their anti-hyperglycaemic activity in glucose-fed hyperglycaemic normal rats. Twenty-three compounds (III-XI, XIV-XVII, XIX-XXIV, XXVI and XXVIII-XXX) showed more or comparable area under the curve (AUC...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Yaseen R,Pushpalatha H,Reddy GB,Ismael A,Ahmed A,Dheyaa A,Ovais S,Rathore P,Samim M,Akthar M,Sharma K,Shafi S,Singh S,Javed K

更新日期：2016-12-01 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：:The discovery of antibiotics as specific and effective drugs against infectious agents has generated the belief that the famous Paul Erlich theory on magic bullet should be applied to cancer as well. However, after around 60 years of failures in finding a magic bullet against cancer, a question appears mandatory: does...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Fais S

更新日期：2016-12-01 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：:We investigated the antioxidant and enzyme inhibitory activities and chemical composition of the hydro-distilled essential oil (0.35% yield) from aerial parts of Thymus spathulifolius. Antioxidant capacity of the oil was assessed by different methods including free radical scavenging (DPPH and ABTS), reducing power (F...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ceylan R,Zengin G,Uysal S,Ilhan V,Aktumsek A,Kandemir A,Anwar F

更新日期：2016-12-01 00:00:00

abstract：:Sulfonamide-bearing thiazole compounds were synthesized and their inhibitory effects on the activity of purified human carbonic anhydrase I and II were evaluated. Human carbonic anhydrase isoenzymes (hCA-I and hCA-II) were purified from erythrocyte cells by affinity chromatography. The inhibitory effects of the 12 syn...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kılıcaslan S,Arslan M,Ruya Z,Bilen Ç,Ergün A,Gençer N,Arslan O

更新日期：2016-12-01 00:00:00

abstract：:Melatonin (MLT) is a well-known free-radical scavenger, involving in the prevention of cellular damage that can lead to cancer, ageing and a variety of neurodegenerative diseases. Research on MLT-related compounds has been required to optimise the maximum pharmaceutical activity with the lowest side effects. In our on...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Shirinzadeh H,Ince E,Westwell AD,Gurer-Orhan H,Suzen S

更新日期：2016-12-01 00:00:00

abstract：:A recombinant carbonic anhydrase (CA, EC 4.2.1.1) from the soil-dwelling bacterium Enterobacter sp. B13 was cloned and purified by Co(2+) affinity chromatography. Bioinformatic analysis showed that the new enzyme (denominated here B13-CA) belongs to the β-class CAs and to possess 95% homology with the ortholog enzyme ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Eminoğlu A,Vullo D,Aşık A,Çolak DN,Supuran CT,Çanakçı S,Osman Beldüz A

更新日期：2016-12-01 00:00:00

abstract：:In the present work, 12 new 2-(5-substituted-benzothiazol-2-ylsulfanyl)-N-(substitutedbenzyl)-N-(4-substitutedphenyl) acetamide derivatives (4a-l) was designed and synthesized. The structures of the synthesized compounds were clarified using Fourier transform infrared spectroscopy (FTIR), proton nuclear magnetic reson...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kaya B,Sağlık BN,Levent S,Özkay Y,Kaplancıklı ZA

更新日期：2016-12-01 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：:Drug target interactions (DTIs) are crucial in pharmacology and drug discovery. Presently, experimental determination of compound-protein interactions remains challenging because of funding investment and difficulties of purifying proteins. In this study, we proposed two in silico models based on support vector machin...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Shar PA,Tao W,Gao S,Huang C,Li B,Zhang W,Shahen M,Zheng C,Bai Y,Wang Y

更新日期：2016-12-01 00:00:00

abstract：:Synthesis and anticonvulsant properties of 26 new N-Mannich bases of 3-benzhydryl-(5-17) and 3-isopropyl-pyrrolidine-2,5-diones (18-30) have been described. Initial anticonvulsant screening for these compounds was evaluated in mice after intraperitoneal administration in the maximal electroshock (MES) and subcutaneous...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Rybka S,Obniska J,Rapacz A,Filipek B,Żmudzki P

更新日期：2016-12-01 00:00:00

abstract：:Resveratrol is a natural polyphenol with plethora of biological activities. Resveratrol has previously shown to decrease DNA-methyltransferase (DNMT) enzymes expression and to reactivate silenced tumor suppressor genes. Currently, it seems that no resveratrol analogs have been developed as DNMT inhibitors. Recently, w...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Aldawsari FS,Aguayo-Ortiz R,Kapilashrami K,Yoo J,Luo M,Medina-Franco JL,Velázquez-Martínez CA

更新日期：2016-10-01 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：:The acetylcholinesterase inhibitory and/or antitumour activities of amino-, thio- and ester-derivatives of avarol selected were evaluated for the first time at in vitro conditions. Avarol-3',4'-dithioglycol (1) and avarol-4'-(3)mercaptopropionic acid (3) were shown to be the best inhibitors of the enzyme tested (0.50 ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Tommonaro G,Pejin B,Iodice C,Tafuto A,De Rosa S

更新日期：2016-08-01 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：:The limited arsenal of synthetic antifungal agents and the emergence of resistant Candida strains have prompted the researchers towards the investigation of naturally occurring compounds or their semisynthetic derivatives in order to propose new innovative hit compounds or new antifungal combinations endowed with redu...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Carradori S,Chimenti P,Fazzari M,Granese A,Angiolella L

更新日期：2016-01-01 00:00:00

abstract：:A set of novel quinolone-triazole conjugates (12-31) were synthesized in three steps in good yields starting from 2-phenylquinoline-4-carboxylic acid. All the intermediates, as well as the final 1,2,4-triazolyl quinolines were fully characterized by their detailed spectral analysis utilizing different techniques such ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Verbanac D,Malik R,Chand M,Kushwaha K,Vashist M,Matijašić M,Stepanić V,Perić M,Paljetak HČ,Saso L,Jain SC

更新日期：2016-01-01 00:00:00

abstract：:Continuous efforts to identify sEH inhibitors using activity-guided fractionation have revealed 12 known compounds, 2-13, from Rheum undulatum. Compounds 2-13 and 1, which was obtained from the in-house library, were tested for inhibitory activity against sEH. Compounds 1-9, 11, and 12 were shown to have inhibitory ac...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Jo AR,Kim JH,Yan XT,Yang SY,Kim YH

更新日期：2016-01-01 00:00:00

abstract：:This study investigates the effect of three new platinum complexes: Pt2(2,4-dimethylpyridine)4(berenil)2 (Pt14), Pt2(3,4-dimethylpyridine)4(berenil)2 (Pt15) and Pt2(3,5-dimethylpyridine)4(berenil)2 (Pt16) on growth and viability of breast cancer cells and their putative mechanism(s) of cytotoxicity. Cytotoxicity was m...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Czarnomysy R,Bielawski K,Muszynska A,Bielawska A,Gornowicz A

更新日期：2016-01-01 00:00:00

abstract：:New ureido benzenesulfonamides incorporating a GABA moiety as a linker between the ureido and the sulfonamide functionalities were synthesized and their inhibition potency determined against both the predominant cytosolic (hCA I and II) and the transmembrane tumor-associated (hCA IX and XII) isoforms of the metalloenz...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ceruso M,Antel S,Scozzafava A,Supuran CT

更新日期：2016-01-01 00:00:00