Quinoline-based imidazole-fused heterocycles as new inhibitors of 15-lipoxygenase.

abstract：:The mechanism of inhalation anesthesia remains to be fully elucidated. While certain neuronal membrane proteins are considered sites of action, cytosolic proteins may also be targets. We hypothesize that inhaled anesthetics may act via glyceraldehyde 3-phosphate dehydrogenase (GAPDH), which has recently been shown to ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Swearengin TA,Fibuch EE,Seidler NW

更新日期：2006-10-01 00:00:00

abstract：:Berberine was investigated as an inhibitor of human protein tyrosine phosphatase 1B (h-PTP 1B) in an attempt to explain its anti-hyperglycemic activitiy. The investigation included simulated docking experiments to fit berberine within the binding pocket of h-PTP 1B. Berberine was found to readily fit within the bindin...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Bustanji Y,Taha MO,Yousef AM,Al-Bakri AG

更新日期：2006-04-01 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：: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：:This research investigates the synthesis and inhibitory potency of a series of novel dipeptidyl allyl sulfones as clan CA cysteine protease inhibitors. The structure of the inhibitors consists of a R(1)-Phe-R(2)-AS-Ph scaffold (AS = allyl sulfone). R(1) was varied with benzyloxycarbonyl, morpholinocarbonyl, or N-methy...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Fennell BD,Warren JM,Chung KK,Main HL,Arend AB,Tochowicz A,Götz MG

更新日期：2013-06-01 00:00:00

abstract：:The bromodomain and extra-terminal (BET) bromodomains, particularly BRD4, have been identified as promising therapeutic targets in the treatment of many human disorders such as cancer, inflammation, obesity, and cardiovascular disease. Recently, the discovery of novel BRD4 inhibitors has garnered substantial interest....

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Zhang Z,Gu L,Wang B,Huang W,Zhang Y,Ma Z,Zeng S,Shen Z

更新日期：2019-12-01 00:00:00

abstract：:This study reports on a preliminary structure-activity relationship exploration of 4-aryliden-2-methyloxazol-5(4H)-one-based compounds as MAGL/FAAH inhibitors. Our results highlight that this scaffold may serve for the development of selective MAGL inhibitors. A 69-fold selectivity against MAGL over FAAH was achieved ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Granchi C,Rizzolio F,Bordoni V,Caligiuri I,Manera C,Macchia M,Minutolo F,Martinelli A,Giordano A,Tuccinardi T

更新日期：2016-01-01 00:00:00

abstract：:Trypanothione reductase (TR) is a major enzyme in trypanosomatids. Its substrate, trypanothione is a molecule containing a tripeptide (L-glutamic acid-cysteine-glycine) coupled to a polyamine, spermidine. This redox system (TR/Trypanothione) is vital for parasite survival within the host cell and has been described as...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Castro-Pinto DB,Lima EL,Cunha AS,Genestra M,De Léo RM,Monteiro F,Leon LL

更新日期：2007-02-01 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：: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：: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：:A series of Co(II), Ni(II) and Cu(II) complexes have been synthesized by template condensation of 2,6-diformyl-4-methylphenol and 3-substituted-4-amino-5-hydrazino-1,2,4-triazole with CoCl(2).6H(2)O, NiCl(2).6H(2)O and CuCl(2).2H(2)O chlorides in 2 + 2+2 molar ratio in ethanol. These complexes were characterized by el...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Avaji PG,Patil SA

更新日期：2009-02-01 00:00:00

abstract：:Three series of sintenin derivatives (compounds 1-14) were designed and prepared and their antioxidative and neuroprotective effects were evaluated. The in vitro models of scavenging 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals, chelating ferrous ions, inhibiting the rat brain homogenates lipid peroxidation, and prot...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Yang LX,Zhang LJ,Huang KX,Kun Li X,Hu LH,Wang XY,Stockigt J,Zhao Y

更新日期：2009-04-01 00:00:00

abstract：:Carbonic anhydrases (CAs, EC 4.2.1.1) are crucial metalloenzymes that are involved in diverse bioprocesses. We report the synthesis and biological evaluation of novel series of benzenesulfonamides incorporating un/substituted ethyl quinoline-3-carboxylate moieties. The newly synthesised compounds were in vitro evaluat...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Al-Sanea MM,Elkamhawy A,Paik S,Bua S,Ha Lee S,Abdelgawad MA,Roh EJ,Eldehna WM,Supuran CT

更新日期：2019-12-01 00:00:00

abstract：:In order to understand the binding modes of human DNA polymerase alpha (pol alpha) inhibitors on a molecular level, a 3D homology model of the active site of the enzyme was proposed based on the application of molecular modelling methods and molecular dynamic simulations using available crystal coordinates of pol alph...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Richartz A,Höltje M,Brandt B,Schäfer-Korting M,Höltje HD

更新日期：2008-02-01 00:00:00

abstract：:In a new group of 3-methyl-2-phenyl-1-substituted-indole derivatives (10a-f), the indomethacin analogs were prepared via the Fisher indole synthesis reaction of propiophenone with appropriately substituted phenylhydrazine hydrochloride. This is followed by the insertion of the appropriate benzyl or benzoyl fragment. A...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Abdellatif KR,Lamie PF,Omar HA

更新日期：2016-01-01 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：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：: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：: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

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：: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：: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：:The in vitro effects of the injectable form of analgesic drugs, dexketoprofen trometamol, dexamethasone sodium phosphate, metamizole sodium, diclofenac sodium, thiocolchicoside, on the activity of purified human carbonic anhydrase I and II were evaluated. The effect of these drugs on erythrocyte hCA I and hCA II was c...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Gökçe B,Gençer N,Arslan O,Turkoğlu SA,Alper M,Köçkar F

更新日期：2012-02-01 00:00:00

abstract：:The α-glucosidase inhibitory activities of bergenin derivatives were evaluated. Bergenin derivatives were synthesized from bergenin which is a characteristic compound of B. ligulata. A new bergenin derivative, 11-O-(3',4'-dimethoxybenzoyl)-bergenin showed the highest potent inhibitory activity among those of bergenin ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kashima Y,Yamaki H,Suzuki T,Miyazawa M

更新日期：2013-12-01 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：: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：:Structure modification of the side chain of the lead compound benzoxanthone provided a series of benzoxanthone analogues and 12 of them were first reported. The results showed that most of these compounds had moderate cytotoxicity against tumour cells with the 50% inhibition concentration in the micromolar range. Furt...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Cheng P,Zhu L,Guo W,Liu W,Yao J,Dong G,Zhang Y,Zhuang C,Sheng C,Miao Z,Zhang W

更新日期：2012-06-01 00:00:00

abstract：:To develop multifunctional aldose reductase (AKR1B1) inhibitors for anti-diabetic complications, a novel series of 2-phenoxypyrido[3,2-b]pyrazin-3(4H)-one derivatives were designed and synthesised. Most of the derivatives were found to be potent and selective against AKR1B1, and 2-(7-chloro-2-(3,5-dihydroxyphenoxy)-3-...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Hao X,Qi G,Ma H,Zhu C,Han Z

更新日期：2019-12-01 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