Synthesis and characterization of some hydroxypyridone derivatives and their evaluation as antimicrobial agents.

abstract：:For the development of potent novel antileishmanial agents, 3,3'-(arylmethylene)bis(2-hydroxynaphthalene-1,4 dione) derivatives were synthesized from lawsone and evaluated for cytotoxicity on Leishmania donovani promastigotes as well as on leishmanial DNA topoisomerase-I. Enzyme inhibition studies were conducted with ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Sharma G,Chowdhury S,Sinha S,Majumder HK,Kumar SV

更新日期：2014-04-01 00:00:00

abstract：:Microbial resistance to the available drugs poses a serious threat in modern medicine. We report the design, synthesis and in vitro antimicrobial evaluation of new functionalized 2,3-dihydrothiazoles and 4-thiazolidinones tagged with sulfisoxazole moiety. Compound 8d was most active against Bacillis subtilis (MIC, 0.0...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Nasr T,Bondock S,Eid S

更新日期：2016-01-01 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：: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：: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：: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：:Histone demethylation is a vital process in epigenetic regulation of gene expression. A number of histone demethylases are present to control the methylated states of histone. Among these enzymes, KDM4s are one subfamily of JmjC KDMs and play important roles in both normal and cancer cells. The discovery of KDM4s inhi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Lin H,Li Q,Li Q,Zhu J,Gu K,Jiang X,Hu Q,Feng F,Qu W,Chen Y,Sun H

更新日期：2018-12-01 00:00:00

abstract：:The flip regression procedure that we used earlier for handling the xanthones system has been applied to phenylaminoquinazoline analogues. It is known that the substituents at the 6- and 7- positions of the polycyclic system have been identified as the most important structural features. The steric as well as the elec...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Deeb O,Clare BW

更新日期：2008-12-01 00:00:00

abstract：:We performed kinetic studies to determine whether oxamate analogues are selective inhibitors of LDH-C4, owing to their potential usefulness in fertility control and treatment of some cancers. These substances were shown to be competitive inhibitors of LDH isozymes and are able to discriminate among subtle differences ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Rodríguez-Páez L,Chena-Taboada MA,Cabrera-Hernández A,Cordero-Martínez J,Wong C

更新日期：2011-08-01 00:00:00

abstract：:17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) is a key enzyme in the biosynthesis of 17β-estradiol. Novel estrone-based compounds bearing various 15β-oxa-linked substituents and hydroxy, methoxy, benzyloxy, and sulfamate groups in position C3 as potential 17β-HSD1 inhibitors have been synthesized. In addition, in...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Herman BE,Kiss A,Wölfling J,Mernyák E,Szécsi M,Schneider G

更新日期：2019-12-01 00:00:00

abstract：:A small library of phosphorylated sulfamates (N-(O-alkylsulfamoyl)-phosphoramidic acids) incorporating long aliphatic chains (C8-C16) has been synthesized and investigated for their interaction with two physiologically relevant carbonic anhydrase (CA) isozymes. These compounds behaved as very potent inhibitors of both...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Bonnac L,Innocenti A,Winum JY,Casini A,Montero JL,Scozzafava A,Barragan V,Supuran CT

更新日期：2004-06-01 00:00:00

abstract：:Human inosine 5'-monophosphate dehydrogenase 2 (hIMPDH2), being an age-old target, has attracted attention recently for anticancer drug development. Mycophenolic acid (MPA), a well-known immunosuppressant drug, was used a lead structure to design and develop modestly potent and selective analogues. The steep structure...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Shah CP,Kharkar PS

更新日期：2018-12-01 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：: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 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 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：: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：: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：:In our endeavour towards the development of effective anticancer therapeutics, a novel series of isoxazole-piperazine hybrids were synthesized and evaluated for their cytotoxic activities against human liver (Huh7 and Mahlavu) and breast (MCF-7) cancer cell lines. Within series, compounds 5l-o showed the most potent c...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Çalışkan B,Sinoplu E,İbiş K,Akhan Güzelcan E,Çetin Atalay R,Banoglu E

更新日期：2018-12-01 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：:The present study describes the synthesis of a series of new 4-aminoquinoline-derived thiazolidines and evaluation of their antimalarial activity against a NF-54 strain of Plasmodium falciparum in vitro and N-67 strain of Plasmodium yoelii in vivo. Among the series, two compounds, 2-(4-chloro-phenyl)-thiazolidine-4-ca...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Solomon VR,Haq W,Srivastava K,Puri SK,Katti SB

更新日期：2013-06-01 00:00:00

abstract：:Phytochemical investigations on the chloroform and ethyl acetate soluble fractions of the roots of Ranunculus repens led to the isolation of methyl 3,4,5-trihydroxybenzoate 1, R(+)- 4-methoxydalbergione 2 and R(+)-dalbergiophenol 3. The structures of these compounds were established through spectral studies including ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Khan WN,Lodhi MA,Ali I,Azhar-Ul-Haq,Malik A,Bilal S,Gul R,Choudhary MI

更新日期：2006-02-01 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：:In this study, di(2,6-dimethylphenol) (Di-DMP), di(2,6-diisopropylphenol) (Di-DIP, dipropofol) and di(2,6-di-t-butylphenol) (Di-DTP) were synthesized by the reaction of monomeric phenol derivatives with catalytic CuCl(OH). TMEDA and Na2S2O4. Their antioxidant capacity and radical scavenging activity were examined usin...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Güllçin I,Daştan A

更新日期：2007-12-01 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：: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：:Corticosteroids are anti-inflammatory drugs that are similar to the natural corticosteroid hormones produced by the cortex of the adrenal glands. The objective of this study was to scrutinize effects of some corticosteroids on glucose-6-phosphate dehydrogenase (G6PD) and some antioxidant enzymes. Initially, G6PD was p...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ozmen I

更新日期：2005-02-01 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：:Histidinol dehydrogenase (HDH, EC EC1.1.1.23) catalyses the final step in the biosynthesis of histidine and constitutes an attractive novel target for the development of new agents against the pathogenous, bacteria Brucella suis. A small library of new HDH inhibitors based on the L-histidinylphenylsulfonyl hydrazide s...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Abdo MR,Joseph P,Boigegrain RA,Montero JL,Köhler S,Winum JY

更新日期：2008-06-01 00:00:00

abstract：:Pig kidney diamine oxidase (DAO) and other semicarbazide-sensitive amine oxidases (SSAO) show clear substrate-inhibition kinetics and a reaction-scheme mechanism based on two substrate binding sites. We evaluated several reaction scheme mechanisms with a non-linear regression program (NCSS), estimating R2, the constan...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ignesti G

更新日期：2003-12-01 00:00:00