Resorcinol-, catechol- and saligenin-based bronchodilating β2-agonists as inhibitors of human cholinesterase activity.

abstract：:The reaction mechanism of glycoside hydrolases belonging to family 1 (GH1) of carbohydrate-active enzymes classification, hydrolysing β-O-glycosidic bonds, is well characterised. This family includes several thousands of enzymes with more than 20 different EC numbers depending on the sugar glycone recognised as substr...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Strazzulli A,Perugino G,Mazzone M,Rossi M,Withers SG,Moracci M

更新日期：2019-12-01 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：:Epidermal growth factor receptor (EGFR) and vascular endothelial growth factor receptor-2 (VEGFR-2), two protein tyrosine kinases, are involved in pathological disorders and the progression of different types of carcinomas. Concomitant inhibition of both tyrosine kinase activities appears to be an attractive target fo...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Garofalo A,Goossens L,Lemoine A,Farce A,Arlot Y,Depreux P

更新日期：2010-04-01 00:00:00

abstract：:A quantitative structure-activity relationship analysis was conducted on two different series of pyridinylguanidines acting as inhibitors of urokinase-type plasminogen activator using QuaSAR descriptors of molecular modeling software MOE. Multiple linear regression analysis following a stepwise scheme was employed to ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Karthikeyan C,Moorthy NS,Trivedi P

更新日期：2009-02-01 00:00:00

abstract：:Neurodegenerative disorders are consequences of progressive and irreversible loss of neurons due to unwanted apoptosis which involves caspases, a group of cysteine proteases that cleave other proteins and inactivate them. Among several different groups of caspase enzymes, caspases-3 plays a key role in apoptosis and a...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Sharma S,Ravichandran V,Jain PK,Mourya VK,Agrawal RK

更新日期：2008-06-01 00:00:00

abstract：:Carbonic anhydrases (CAs, EC 4.2.1.1) are ubiquitous enzymes that catalyze the hydration of CO(2) to bicarbonate and protons. Inhibition of CAs has been clinically exploited for the treatment of various classes of diseases for decades, but investigating new classes of inhibitors continues to be important. We have synt...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ayvaz S,Çankaya M,Atasever A,Altuntas A

更新日期：2013-04-01 00:00:00

abstract：:Nitrofurazone (NF) and its derivative, hydroxymethylnitrofurazone (NFOH), have presented antichagasic activity. NFOH has higher activity and lower mutagenicity. The aim of this work was to assess whether NF and its derivative NFOH would also be inhibitors of cruzain, besides their trypanothione reductase inhibitory ac...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Trossini GH,Malvezzi A,T-do Amaral A,Rangel-Yagui CO,Izidoro MA,Cezari MH,Juliano L,Chin CM,Menezes CM,Ferreira EI

更新日期：2010-02-01 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 small and highly electronegative fluorine atom can play a remarkable role in medicinal chemistry. Selective installation of fluorine into a therapeutic or diagnostic small molecule candidate can enhance a number of pharmacokinetic and physicochemical properties such as improved metabolic stability and enhanced mem...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Shah P,Westwell AD

更新日期：2007-10-01 00:00:00

abstract：:[60]Fullerene-peptides represent a simple yet chemically diverse example of a bio-nano conjugate. The C60 moiety provides the following attributes to the conjugate: (a) precise three-dimensional architecture, (b) a large hydrophobic mass and (c) unique electronic properties. Conversely, the peptide component provides:...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Barron AR

更新日期：2016-01-01 00:00:00

abstract：:A new series of functionalized amino acid derivatives N-substituted 1-N-(tert-butoxycarbonyl)-2,2-dimethyl-4-phenyl-5-oxazolidine carboxamide (1-17) and 1-N-substituted-3-amino-2-hydroxy-3-phenylpropane-1-carboxamide (18-34) were synthesized and evaluated for their in vitro cytotoxicity against human cancer cell lines...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kumar V,Mudgal MM,Rani N,Jha A,Jaggi M,Singh AT,Sanna VK,Singh P,Sharma PK,Irchhaiya R,Burman AC

更新日期：2009-06-01 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：:Initial velocity enzyme kinetics was used to study the inhibition mechanism of guanidine hydrochloride (Gdm.Cl) on catalytic activity of recombinant human protein disulfide isomerase (rhPDI) in protein folding. Reduced C125A recombinant human interleukin 2 (C125A rhIL-2), the substrate, was dissolved in 8 M Gdm.Cl bef...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Du C,Wolfe JL

更新日期：2003-02-01 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：:Two new series of heterocyclic derivatives with potential anticancer activity, in which a pyrrolo[1,2-b]pyridazine or a pyrrolo[2,1-a]phthalazine moiety was introduced in place of the 3'-hydroxy-4'-methoxyphenyl ring of phenstatin have been synthesised and their structure-activity relationship (SAR) was studied. Fourt...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Popovici L,Amarandi RM,Mangalagiu II,Mangalagiu V,Danac R

更新日期：2019-12-01 00:00:00

abstract：:To identify anticancer agents with high potency and low toxicity, a series of (Z)-styrylbenzene derivatives were synthesised and evaluated for anticancer activities using a panel of nine cancer cell lines and two noncancerous cell lines. Most derivatives exhibited significant anti-proliferative activities against five...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Xin YB,Li JJ,Zhang HJ,Ma J,Liu X,Gong GH,Tian YS

更新日期：2018-12-01 00:00:00

abstract：:This study presents the synthesis and in vitro pharmacological evaluations of novel 2-(4-cyanophenyl amino)-4-(6-bromo-4-quinolinyloxy)-6-piperazinyl (piperidinyl)-1,3,5-triazines. The title compounds were assayed for their in vitro antimicrobial activity against eight bacteria (Staphylococcus aureus, Bacillus cereus,...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Patel RV,Kumari P,Rajani DP,Chikhalia KH

更新日期：2012-06-01 00:00:00

abstract：:The needs for diverse inhibitors of α-glucosidase (α-Gls) encouraged us to synthesize five different poly-hydroxy functionalized pyrimidine-fused heterocyclic (PHPFH) molecules, having either aliphatic or aromatic side chains (C1-C5) and their inhibitory activities were examined spectroscopically against yeast and mou...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Yousefi R,Alavian-Mehr MM,Mokhtari F,Panahi F,Mehraban MH,Khalafi-Nezhad A

更新日期：2013-12-01 00:00:00

abstract：:In this work, we reported the synthesis and evaluation of antibacterial and antifungal activities of three new compound series obtained from 6-(phenyl/4-chlorophenyl)imidazo[2,1-b]thiazole-3-acetic acid hydrazide: 2-{[6-(phenyl/4-chlorophenyl)imidazo[2,1-b]thiazol-3-yl]acetyl}-N-alkyl/arylhydrazinecarbothioamides (2a-...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Güzeldemirci NU,Satana D,Küçükbasmacı O

更新日期：2013-10-01 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：: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：:EGFR tyrosine kinase has been reported mainly in 40-80% of non-small lung cancers, in addition to colon and breast cancers. In this study, we illustrate the synthesis of a highly potent antitumor agent. The synthesized compound 4 was screened at NCI, USA, for antitumor activity against non-small lung cancer, colon can...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Gabr MT,El-Gohary NS,El-Bendary ER,El-Kerdawy MM

更新日期：2015-02-01 00:00:00

abstract：:In the present study, some thiazole derivatives were synthesized via the ring closure reaction of 1-[2-(2-oxobenzo[d]thiazol-3(2H)-yl)acetyl]thiosemicarbazide with various phenacyl bromides. The chemical structures of the compounds were elucidated by (1)H NMR, (13)C NMR and mass spectral data and elemental analyses. E...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Turan-Zitouni G,Ozdemir A,Kaplancikli ZA,Altintop MD,Temel HE,Çiftçi GA

更新日期：2013-06-01 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：: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：: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：:The results of extensive quantitative structure-activity relationship (QSAR) analyses on 15 series of cytochrome P450 inhibitors, covering a total of 7 enzymes and 199 compounds, are reported. In general, it is found that lipophilicity represents the most important single factor in describing differences in inhibitory...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Lewis DF,Lake BG,Dickins M

更新日期：2007-02-01 00:00:00

abstract：:Early stages of avascular necrosis of the femoral head (AVNFH) can be conservatively treated with hyperbaric oxygen therapy (HBOT). This study investigated how HBOT modulates inflammatory markers and reactive oxygen species (ROS) in patients with AVNFH. Twenty-three male patients were treated with two cycles of HBOT, ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Bosco G,Vezzani G,Mrakic Sposta S,Rizzato A,Enten G,Abou-Samra A,Malacrida S,Quartesan S,Vezzoli A,Camporesi E

更新日期：2018-12-01 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：: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