New indolesulfonamide derivatives targeting the colchicine site of tubulin: synthesis, anti-tumour activity, structure-activity relationships, and molecular modelling.

abstract：:The invertase inhibitory protein isolated from Cyphomandra betacea Sendt and Solanum tuberosum inhibited the invertase activity from different species, genera and even plant family. Furthermore, proteinaceous inhibitors are not invertase specific; fungal, bacterial and higher plant enzymes including polygalacturonase,...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Isla MI,Ordóñez RM,Moreno MI,Sampietro AR,Vattuone MA

更新日期：2002-02-01 00:00:00

abstract：:An acid invertase from the fern Pteris deflexa Link was purified and the effect of reaction products on enzyme activity was studied. Fructose and glucose were competitive and non-competitive inhibitors of the enzyme, respectively. Since proteins suppressed glucose and fructose inhibition of the enzyme, an invertase mo...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Sayago JE,Vattuone MA,Sampietro AR,Isla MI

更新日期：2002-04-01 00:00:00

abstract：:Condensation reactions of 1,1''-diacetylferrocene with different heteroaromatic amines such as, 2-amino-1,3,4-thiadiazole, 5-aminotetrazole and 3-amino-1,2,4-triazole to form unsymmetrically 1,1'-disubstituted ferrocenes have been studied. The obtained compounds have been further investigated for their liganding and b...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Chohan ZH,Scozzafava A,Supuran CT

更新日期：2002-08-01 00:00:00

abstract：:The goal of the present study was to evaluate several azolyl-substituted indoles as new antileishmanial agents. Ten 3-(alpha-azolylbenzyl)indoles have been synthesized using Friedel-Crafts acylation as a key-step. All the target compounds were found to display high levels of activity when tested against Leishmania mex...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Marchand P,Le Borgne M,Na YM,Pagniez F,Abdala H,Le Baut G,Le Pape P

更新日期：2002-12-01 00:00:00

abstract：:A new 2-(alpha-azolylbenzyl)indole derivative exhibited high in vitro activity against 10 strains of Aspergillus fumigatus. This active compound, MT18n, had MIC of 2 microg/mL and is slightly less active than itraconazole and amphotericin B. The mechanism of action of this compound was evaluated through scanning elect...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Pagniez F,Le Borgne M,Marchand P,Na YM,Le Baut G,Robert-Piessard S,Le Pape P

更新日期：2002-12-01 00:00:00

abstract：:To determine the catalytic site of Streptomyces chromofuscus phospholipase D (PLD), which lacks an HKD motif, we examined the effects of inhibitors on the hydrolytic activity of the PLD by comparing it with cabbage and Streptomyces PLDs, which have two HKD motifs. We showed that dichloro-(2,2':6',2''-terpyridine)-plat...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kubota-Akizawa M,Negishi T,Mori K,Hatanaka T

更新日期：2002-10-01 00:00:00

abstract：:A series of 5-[1-(2-haloethyl(or nitro)ethoxy-2-iodoethyl)]-2'-deoxyuridines (3-7) and related uracil analogs (9-10) were prepared using 5-vinyl-2-deoxyuridine (2) and 5-vinyl uracil (8) as starting materials. The regiospecific reaction of 2 and 8 with iodine monochloride and an alcohol provided the target compounds 3...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Rai D,Saffran H,Kumar R

更新日期：2003-02-01 00:00:00

abstract：:Among a library of 70 azoles, 8 indole derivatives substituted in the 2-, 3- or 5- position with an azolylmethyl or alpha-azolylbenzyl chain were evaluated for retinoic acid (RA) metabolism inhibitory activity. The most active inhibitors identified in this study were 5-bromo-1-ethyl-3-methyl-2-[(phenyl)(1H-1,2,4-triaz...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Le Borgne M,Marchand P,Le Baut G,Ahmadi M,Smith HJ,Nicholls PJ

更新日期：2003-04-01 00:00:00

abstract：:The 5-halo-6-methoxy-5,6-dihydro derivatives of 5-[1-methoxy-2-halo(or 2,2-dihalo)ethyl]-2'-deoxyuridines (3-12) were synthesized and investigated as potential anti-herpes agents. These 5,6-dihydro derivatives were designed to act as potential prodrugs to 5-[1-methoxy-2-halo(or 2,2-dihalo)ethyl]-2'-deoxyuridines (2a-e...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kumar R

更新日期：2003-06-01 00:00:00

abstract：:(+/-)-4-Methylthioamphetamine (MTA) was resolved into its enantiomers, and a series of N-alkyl derivatives of the parent compound, as well as its alpha-ethyl analogue, were prepared. The monoamine oxidase (MAO) inhibitory properties of these substances were evaluated in vitro, using a crude rat brain mitochondrial sus...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Hurtado-Guzmán C,Fierro A,Iturriaga-Vásquez P,Sepúlveda-Boza S,Cassels BK,Reyes-Parada M

更新日期：2003-08-01 00:00:00

abstract：:Allicin--diallyl thiosulfinate--is the main biologically active component of freshly crushed garlic. Allicin was synthesized as described elsewhere and was tested for its inhibitory ability against jack bean urease in 20 mM phosphate buffer, pH 7.0 at 22 degrees C. The results indicate that allicin is an enzymatic ina...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Juszkiewicz A,Zaborska W,Sepioł J,Góra M,Zaborska A

更新日期：2003-10-01 00:00:00

abstract：:The effects of gentamicin sulphate, thiamphenicol, ofloxacin, levofloxacin, cefepime, and cefazolin were investigated on the in vitro enzyme activity of glutathione reductase. The enzyme was purified 1,850-fold with a yield 18.76% from sheep liver using ammonium sulphate precipitation, 2',5'-ADP Sepharose 4B affinity ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Erat M,Ciftçi M

更新日期：2003-12-01 00:00:00

abstract：:Inhibition of CYP 17 is a promising strategy for the treatment of prostate cancer. Recently two non-steroidal compounds with high in vitro activity were synthesized in our group (BW19 and BW95). However, after a few hours they showed in vivo a strong decrease in their activity. This might be due to a fast biodegradati...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Hutschenreuter TU,Ehmer PB,Hartmann RW

更新日期：2004-02-01 00:00:00

abstract：:Muscle-type LDH (LDH-m4) activity is critical for efficient anaerobic glycolysis. The results here show that rabbit LDH-M4 is inhibited by concentrations of ascorbate normally found in tissues. Aldolase and muscle G-actin were found to protect and to reverse inhibitions of LDH-m4 by ascorbate. G-actins showed some spe...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Russell PJ,Williams A,Amador X,Vargas R

更新日期：2004-02-01 00:00:00

abstract：:Regioselectively fluorinated 1-(naphth-2-ylmethyl)imidazoles 1a-h have been synthesized starting from the corresponding (naphth-2-yl)methanols (2). 2a-d have been obtained by LiAlH4-promoted reduction of fluorinated 1-methyl-2-naphthaldehydes. The latter were easily prepared in fairly good overall yields by ceric ammo...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Hartmann RW,Palusczak A,Lacan F,Ricci G,Ruzziconi R

更新日期：2004-04-01 00:00:00

abstract：:Benzolamide, an orphan drug belonging to the pharmacological class of sulfonamide carbonic anhydrase (CA, EC 4.2.1.1) inhibitors (CAIs) is widely used in many physiological and pharmacological studies, together with the clinically employed classical drugs, acetazolamide, methazolamide, ethoxzolamide or dichlorophenami...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Supuran CT,Scozzafava A

更新日期：2004-06-01 00:00:00

abstract：:Na+/K+-ATPase (EC 3.6.1.3) is an important membrane-bound enzyme. In this paper, kinetic studies on Na+/K+-ATPase were carried out under mimetic physiological conditions. By using microcalorimeter, a thermokinetic method was employed for the first time. Compared with other methods, it provided accurate measurements of...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Xia L,Yuwen L,Jie L,Huilin L,Xi Y,Cunxin W,Zhiyong W

更新日期：2004-08-01 00:00:00

abstract：:The activity of several diarylheptanoid derivatives (curcuminoids) was previously evaluated against Leishmania amazonensis promastigotes and among them the most active compound was 5-hydroxy-7- (4-hydroxy-3-methoxyphenyl)-1-(4-methoxyphenyl)-1,4,6-heptatrien-3-one. This study was carried out to investigate the influen...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Alves LV,Cysne-Finkelstein L,Temporal RM,Genestra MS,Leon LL

更新日期：2004-10-01 00:00:00

abstract：:New N1-mono and N1, N2-disubstituted imidazolidin-2-one with a significant immunosuppressive activity have been discovered. Among the 17 synthesized and tested compounds, five of them showed maximal inhibition of proliferation of concanavallin A (Con A)- stimulated splenocytes at 90 microM, identical to that obtained ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Sabourin C,Robert JM,Robert-Piessard S,Carbonnelle D,Lang F

更新日期：2004-12-01 00:00:00

abstract：:Fosmidomycin, 3-(N-formyl-N-hydroxyamido) propylphosphonic acid sodium salt, is an efficient inhibitor of 1-deoxy-D-xylulose-5-phosphate (DOXP) reductoisomerase, the second enzyme of the 2C-methyl-D-erythritol-4-phosphate (MEP) pathway notably present in Plasmodium species. We have synthesized a new series of analogue...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Courtois M,Mincheva Z,Andreu F,Rideau M,Viaud-Massuard MC

更新日期：2004-12-01 00:00:00

abstract：:Previous work has demonstrated that N-N'-diphenyl-R-benzamidine was highly effective against Leishmania amazonensis promastigotes/axenic amastigotes and Trypanosoma evansi trypomastigotes and the compound with a methoxy substituent, was the most effective derivative in the parasite-macrophage interaction. Comparative ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Temporal RM,Cysne-Finkelstein L,Echevarria A,Silva-Gonçalves AJ,Leon LL,Genestra MS

更新日期：2005-02-01 00:00:00

abstract：:Organometallic-based, 1,1'-diacetylferrocene-derived antibacterial and antifungal thiocarbohydrazone, carbohydrazone, thiosemicarbazone and semicarbazone have been prepared by condensing equimolar amount of 1,1'-diacetylferrocene with thiocarbohydrazide, carbohydrazide thiosemicarbazide and semicarbazide, respectively...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Chohan ZH,Pervez H,Khan KM,Supuran CT

更新日期：2005-02-01 00:00:00

abstract：:Plant copper/topaquinone-containing amine oxidases (CAOs, EC 1.4.3.6) are enzymes oxidising various amines. Here we report a study on the reactions of CAOs from grass pea (Lathyrus sativus), lentil (Lens esculenta) and Euphorbia characias, a Mediterranean shrub, with N6-aminoalkyl adenines representing combined analog...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Lamplot Z,Sebela M,Frycák P,Longu S,Padiglia A,Medda R,Floris G,Pec P

更新日期：2005-04-01 00:00:00

abstract：:KBrO3-mediated renal injury and hyperproliferative response in Wistar rats. In this communication, we report the efficacy of Nymphaea alba on KBrO3 (125 mg/kg body weight, intraperitoneally) caused reduction in renal glutathione content, renal antioxidant enzymes and phase-II metabolising enzymes with enhancement in x...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Khan N,Sultana S

更新日期：2005-06-01 00:00:00

abstract：:The inhibitory effects of a black tea extract on fatty acid synthase were measured through inhibition kinetics. The Keemun black tea extract showed more potent inhibitory activity on fatty acid synthase than green tea extract. Additionally, the inhibitory ability of the black tea extract depended on the extracting sol...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Du YT,Wang X,Wu XD,Tian WX

更新日期：2005-08-01 00:00:00

abstract：:Intraocular neovascularization is a complication in a variety of eye diseases, and is a leading cause of visual loss. The purpose of this study was to design and synthesize three novel codrugs of the antiangiostatic steroid, 3alpha, 17alpha, 21-trihydroxy-5beta-pregnan-20-one (trihydroxy steroid, THS) with the cytotox...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Howard-Sparks M,Al-Ghananeem AM,Pearson AP,Crooks PA

更新日期：2005-10-01 00:00:00

abstract：:Effects of nicotine, and nicotine + vitamin E on glucose 6-phosphate dehydrogenase (G-6PD) activity in rat muscle, heart, lungs, testicle, kidney, stomach, brain and liver were investigated in vivo and in vitro on partially purified homogenates. Supplementation period was 3 weeks (n = 8 rats per group): nicotine [0.5 ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Gumustekin K,Ciftci M,Coban A,Altikat S,Aktas O,Gul M,Timur H,Dane S

更新日期：2005-10-01 00:00:00

abstract：:We have previously reported the synthesis and evaluation of potent anti-human immunodeficiency virus compounds based on beta-D-d4T analogues bearing a tether attached at the C-5 position and their beta-L-counterparts. Initial study revealed a requirement for an alkyl side-chain with an optimal length of 12 carbons for...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ladurée D,Fossey C,Delbederi Z,Sugeac E,Schmidt S,Laumond G,Aubertin AM

更新日期：2005-12-01 00:00:00

abstract：:Atherosclerosis is one of the most frequent causes of cardiac arrest. The major cause of this disease is high concentrations of lipid in the blood. Medicinal agents so far have been quite successful in the management of hyperlipidemia. Among the several widely used drugs, (fibrates, statins and niacin) statins are the...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Brahmkshatriya PS,Jani MH,Chhabria MT

更新日期：2006-02-01 00:00:00

abstract：:In vitro effects of omeprazole, morphine sulphate, remifentanyl, ketamine and vankomycin were investigated on human red blood cell glucose-6 phosphate dehydrogenase (G-6PD) (E.C. 1.1.1.49) enzyme activity purified from human red blood cell by 2', 5'ADP-Sepharose 4B affinity gel. The obtained I50 values of omeprazole, ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ozdemir H,Ciftçi M

更新日期：2006-02-01 00:00:00