Carbonic anhydrase inhibitors: synthesis of water soluble sulfonamides incorporating a 4-sulfamoylphenylmethylthiourea scaffold, with potent intraocular pressure lowering properties.

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：:Protein disulphide isomerase (PDI) in the endoplasmic reticulum catalyzes the rearrangement of disulphide bridges during folding of secreted proteins. It binds various molecules that inhibit its activity. But here, we looked for molecules that would potentiate its activity. PDI reductase activity was measured in vitro...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Hassan MH,Alvarez E,Cahoreau C,Klett D,Lecompte F,Combarnous Y

更新日期：2011-10-01 00:00:00

abstract：:The design of multi-target directed ligands (MTDLs) is a valid approach for obtaining effective drugs for complex pathologies. MTDLs that combine neuro-repair properties and block the first steps of neurotoxic cascades could be the so long wanted remedies to treat neurodegenerative diseases (NDs). By linking two privi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Estrada-Valencia M,Herrera-Arozamena C,Pérez C,Viña D,Morales-García JA,Pérez-Castillo A,Ramos E,Romero A,Laurini E,Pricl S,Rodríguez-Franco MI

更新日期：2019-12-01 00:00:00

abstract：:The synthesis, in vitro antimicrobial activities of some novel hydroxy pyridines supported with various pharmacophores is described. Twenty-six out of the tested 58 compounds exhibited variable inhibitory effects on the growth of the tested Gram positive and Gram negative bacteria. The tested compounds revealed better...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Faidallah HM,Rostom SA,Khan KA,Basaif SA

更新日期：2013-10-01 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

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：: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：:An efficient and simple microwave assisted synthesis of sulfonamide derivatives incorporating the pyridazine moiety has been developed. These sulfonamides were used for the preparation of new heterocyclic compounds via reaction with different reagents using a microwave irradiation technique. The structures of the newl...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Mohamed MI,Zaky HT,Kandile NG

更新日期：2013-12-01 00:00:00

abstract：:The activation of the β-class carbonic anhydrases (CAs, EC 4.2.1.1) from the bacteria Brucella suis and Francisella tularensis with amine and amino acids was investigated. BsuCA 1 was sensitive to activation with amino acids and amines, whereas FtuCA was not. The most effective BsuCA 1 activators were L-adrenaline and...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Angeli A,Del Prete S,Pinteala M,Maier SS,Donald WA,Simionescu BC,Capasso C,Supuran CT

更新日期：2019-12-01 00:00:00

abstract：:The synthesis of a new series of imidazo[1,2-a]pyrazine-2-carboxylic acid arylidene-hydrazides is described. The chemical structures of the compounds were elucidated by IR, (1)H-NMR, FAB(+)-MS spectral data. Their biological activity against various bacteria, fungi species, and Mycobacterium tuberculosis was investiga...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ozdemir A,Turan-Zitouni G,Kaplancikli ZA,Tunali Y

更新日期：2009-06-01 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：: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 synthesis of 2-isopropenyl-2,3-dihydrobenzofuranic enantioisomers is described. Ortho-(2-hydroxy-3-methyl-but-3-enyl)phenol synthons are used as precursors to these structures. In vitro antitumor activity against a non-small-cell bronchopulmonary carcinoma line (NSCLC-N6) of these enantioisomers has been investiga...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Hélesbeux JJ,Duval O,Séraphin D,Roussakis C,Richomme P

更新日期：2003-04-01 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：: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：:Flavonoids, polyphenolic phytochemicals, are ubiquitous in plants and are commonly present in the human diet. They may exert diverse beneficial effects, including antioxidant and anticarcinogenic activities. The present study was designed to evaluate three biomolecules that play important roles in the apoptotic proces...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： de Sousa RR,Queiroz KC,Souza AC,Gurgueira SA,Augusto AC,Miranda MA,Peppelenbosch MP,Ferreira CV,Aoyama H

更新日期：2007-08-01 00:00:00

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：:Several 2,5-disubstituted-1,3,4-oxadiazoles (4a-f) and 3,6-disubstituted-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazoles (7a-f) were synthesized and characterized by elemental analyses and spectral data. These compounds were screened for their anti-inflammatory, analgesic, ulcerogenic and lipid peroxidation activities. Compo...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Chawla G,Kumar U,Bawa S,Kumar J

更新日期：2012-10-01 00:00:00

abstract：:In this study, the synthesis and potential enzyme interactions of new Pyrrolo[2,3-d]pyrimidine derivatives along with their inhibitory activity against SFK enzymes such as Fyn, Lyn, Hck, and c-Src were reported. The results indicated that compounds were slightly active of tested SFK enzymes in comparison with PP2 for ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Dincer S,Cetin KT,Onay-Besikci A,Ölgen S

更新日期：2013-10-01 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：: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：: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：CONTEXT:Hypotension causes histologic changes in the hippocampal CA1 area, while behavior remains unchanged. We believe that an even stronger insult may also cause behavioral changes. OBJECTIVE:We used a rat hemorrhagic shock model plus temporary hypoxia to assess functional outcome at different time points post-injur...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Chaparro E,Quiroga C,Erasso D,Bosco G,Rubini A,Mangar D,Camporesi E

更新日期：2014-12-01 00:00:00

abstract：:A new series of N-heteroarylsubstituted triazolosulfonamide compounds were synthesized and their inhibitory effects on the activity of purified human carbonic anhydrase (hCA) I and II were evaluated. Compounds (3 a-k) were prepared by propargylation of N-heteroaryl compounds. Compound 5 was obtained from sulfanilamide...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Balci A,Arslan M,Nixha AR,Bilen C,Ergun A,Gençer N

更新日期：2015-06-01 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：: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：:Complexes of the type [M(pabh)(H2O)Cl], [M(pcbh)(H2O)Cl] and [M(Hpabh)(H2O)2 (SO4)] where, M = Mn(II), Co(II), Ni(II), Cu(II) and Zn(II); Hpabh = p-amino acetophenone benzoyl hydrazone and Hpcbh = p-chloro acetophenone benzoyl hydrazone have been synthesized and characterized with the help of elemental analyses, elect...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Singh VP,Singh S,Katiyar A

更新日期：2009-04-01 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

abstract：:Cyanidin-3-galactoside, a natural anthocyanin, was investigated for its alpha-glucosidase inhibitory activity. The IC(50) value of cyanidin-3-galactoside was 0.50 +/- 0.05 mM against intestinal sucrase. A low dose of cyanidin-3-galactoside showed a synergistic inhibition on intestinal alpha-glucosidase (maltase and su...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Adisakwattana S,Charoenlertkul P,Yibchok-Anun S

更新日期：2009-02-01 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