Using C60 fullerenes for photodynamic inactivation of mosquito iridescent viruses.

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：:A series of N1-(substituted)aryl-5,7-dimethyl-2-(substituted)pyrido(2,3-d)pyrimidin-4(3H)-one was designed on the basis of the triangular pharmacophoric requirement of histamine H1-receptor antagonists. The designed series was synthesized by cyclo-condensation of monoaryl thiourea with ethyl cyanoacetate in the presen...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Suhagia BN,Chhabria MT,Makwana AG

更新日期：2006-12-01 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：:Numerous studies have highlighted the implications of the glycogen synthase kinase 3 (GSK-3) in several processes associated with Alzheimer's disease (AD). Therefore, GSK-3 has become a crucial therapeutic target for the treatment of this neurodegenerative disorder. Hereby, we report the design and multistep synthesis...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Sciú ML,Sebastián-Pérez V,Martinez-Gonzalez L,Benitez R,Perez DI,Pérez C,Campillo NE,Martinez A,Moyano EL

更新日期：2019-12-01 00:00:00

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：: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：: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：: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：: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：: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

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：:The aims of this study were to examine the antiproliferation of Humulus lupulus extracts on human hepatoma carcinoma (Hep3B) and human colon carcinoma (HT-29) cell lines along with enzyme inhibitory effects of the crude extracts. Potential cell cytotoxicity of six different H. lupulus extracts were assayed on various ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Cömert Önder F,Ay M,Aydoğan Türkoğlu S,Tura Köçkar F,Çelik A

更新日期：2016-01-01 00:00:00

abstract：:Arylsulfatase B (ASB) hydrolyzes the desulfation of N-acetylgalactosamine-4-sulfate at the non-reducing terminal of glycosaminoglycans. This enzyme activity was found to be elevated in mice schistosomiasis. In the present study, the catalytic and immunological properties of purified ASB from the liver of Schistosoma-i...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Balbaa M,Bassiouny K

更新日期：2006-02-01 00:00:00

abstract：:The CHCl(3)-soluble fraction of the whole plant of Duranta repens showed anti-plasmodial activity against the chloroquine-sensitive (D6) and chloroquine-resistant (W2) strains of Plasmodium falciparum, with IC(50) values of 8.5 ± 0.9 and 10.2 ± 1.5 μg/mL, respectively. From this fraction, two new flavonoid glycosides,...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ijaz F,Ahmad N,Ahmad I,ul Haq A,Wang F

更新日期：2010-12-01 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：:A trypsin inhibitor isolated from tamarind seed (TTI) has satietogenic effects in animals, increasing the cholecystokinin (CCK) in eutrophy and reducing leptin in obesity. We purified TTI (pTTI), characterised, and observed its effect upon CCK and leptin in obese Wistar rats. By HPLC, and after amplification of resolu...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Medeiros AF,Costa IS,Carvalho FMC,Kiyota S,Souza BBP,Sifuentes DN,Serquiz RP,Maciel BLL,Uchôa AF,Santos EAD,Morais AHA

更新日期：2018-12-01 00:00:00

abstract：UNLABELLED:Abstract In biological systems, the Keap1/Nrf2/antioxidant response element pathway determines the ability of mammalian cells to adapt and survive conditions of oxidative, electrophilic and inflammatory stress by regulating the production of cytoprotective enzymes NAD(P)H:quinone oxidoreductase 1 (NQO1, EC ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ghorab MM,Higgins M,Alsaid MS,Arafa RK,Shahat AA,Dinkova-Kostova AT

更新日期：2014-12-01 00:00:00

abstract：:A new series of fluorine containing 1,3,5-triazinyl sulfonamide derivatives obtained from cyanuric fluoride, sulfanilamide/4-aminoethylbenzenesulfonamide followed and incorporating also amin0, amino alcohol and amino acid moieties have been investigated as inhibitors of three β-carbonic anhydrases (CAs, EC 4.2.1.1) fr...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ceruso M,Vullo D,Scozzafava A,Supuran CT

更新日期：2014-10-01 00:00:00

abstract：:A series of benzoic acid derivatives 1-10 have been synthesised by two different methods. Compounds 1-6 were synthesised by a facile procedure for esterification using N,N'-dicyclohexylcarbodiimide (DCC) as a coupling agent, methylene chloride as a solvent system and dimethylaminopyridine (DMAP). While 7-10 were synth...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Khan SB,Hassan Khan MT,Jang ES,Akhtar K,Seo J,Han H

更新日期：2010-12-01 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：: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：: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：: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：: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：:A new series of 12 N(4)-substituted isatin-3-thiosemicarbazones 2a-l has been synthesized, characterized and screened for in vitro cytotoxic, phytotoxic and urease inhibitory effects. All the compounds proved to be active in the brine shrimp bioassay; 2a, 2b, 2d, 2f and 2h-l exhibited a high degree of cytotoxic activi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Pervez H,Chohan ZH,Ramzan M,Nasim FU,Khan KM

更新日期：2009-04-01 00:00:00

abstract：:Inflammatory bowel disease (IBD) is a chronic immuno-inflammation in gastrointestinal tract. We have evaluated the activity of the compounds to inhibit the adhesion of monocytes to colon epithelial cells is triggered by a pro-inflammatory cytokine, tumour necrosis factor (TNF)-α. The in vitro activity of the compounds...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Chaudhary CL,Gurung P,Jang S,Banskota S,Nam TG,Kim JA,Jeong BS

更新日期：2020-12-01 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：:The synthesis and biological evaluation of some novel thiazolofluorenones, thiazolofluorenes and thiazoloanthraquinones, substituted with amino side-chains are described. These polyheterocyclic compounds have been synthesized via the corresponding imino-1,2,3-dithiazoles. Their cytotoxic activity and their eventual se...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Chabane H,Pierre A,Leonce S,Pfeiffer B,Renard P,Thiery V,Guillaumet G,Besson T

更新日期：2004-12-01 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：: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