Design and synthesis of novel quinazolinones conjugated ibuprofen, indole acetamide, or thioacetohydrazide as selective COX-2 inhibitors: anti-inflammatory, analgesic and anticancer activities.

abstract：:Schiff bases derived from oxaldiamide/oxalylhydrazine and pyrrol-2-carbaldehyde, or salicylaldehyde respectively, as well as their Zn(II) complexes have been prepared and tested as antibacterial agents. These Schiff bases function as tetradentate ligands, forming octahedral Zn(II) complexes. The ketonic form for the d...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Chohan ZH,Farooq MA,Scozzafava A,Supuran CT

更新日期：2002-02-01 00:00:00

abstract：:The 7-hydroxycoumarins, umbelliferone and 4-methylumbelliferone (IC50 = 1.4 and 1.9 microM, respectively) were potent inhibitors of human testes microsomal 17beta-HSD (type 3) enzyme whereas 7-methoxycoumarin, 4-hydroxycoumarin and 7-ethoxycoumarin had little or no inhibitory activity. Analogues of the weak inhibitory...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： LE Lain R,Barrell KJ,Saeed GS,Nicholls PJ,Simons C,Kirby A,Smith HJ

更新日期：2002-04-01 00:00:00

abstract：:In search of non-steroidal inhibitors of human prostatic 5alpha-reductase, we recently described N-substituted 4'-biphenyl-4-carboxylic acids. Here, we report the optimisation of this series of compounds by increasing the conformational flexibility using an ether linker between the steroidal A-C ring mimetics. Ten new...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Picard F,Hartmann RW

更新日期：2002-06-01 00:00:00

abstract：:A series of pyrazolo[3,4-d]pyridazinones and analogues, potentially useful as peripheral vasodilators, were synthesized and evaluated as inhibitors of PDE5 extracted from human platelets. Several of them showed IC50 values in the range 0.14-1.4 microM. A good activity and selectivity profile versus PDE6 was found for ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Dal Piaz V,Castellana MC,Vergelli C,Giovannoni MP,Gavaldà A,Segarra V,Beleta J,Ryder H,Palacios JM

更新日期：2002-08-01 00:00:00

abstract：:Novel thiazolocarbazole derivatives 4 and 5 have been synthesized via the corresponding imino-1,2,3-dithiazoles 3. In vitro antitumor activity of these polyheterocyclic compounds was studied and the results show that 2-cyano derivatives exhibit a medium in vitro antiproliferative effect. ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

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

更新日期：2002-12-01 00:00:00

abstract：:A quantitative structure-activity relationship (QSAR) study is made on the inhibition of a few isozymes of carbonic anhydrase (CA) and some matrix metalloproteinases (MMPs), both zinc containing families of enzymes, by sulfonylated amino acid hydroxamates. For both enzymes, the inhibition potency of the hydroxamates i...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Gupta SP,Maheswaran V,Pande V,Kumar D

更新日期：2003-02-01 00:00:00

abstract：:Serotonin N-acetyltransferase (arylalkylamine N-acetyltransferase, AANAT) is the penultimate enzyme in melatonin (5-methoxy-N-acetyltryptamine) biosynthesis. It is the key-enzyme responsible of the nocturnal rhythm of melatonin production in the pineal gland. Specific AANAT inhibitors could be useful for treatment of ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Mesangeau C,Yous S,Chavatte P,Ferry G,Audinot V,Boutin JA,Delagrange P,Bennejean C,Renard P,Lesieur D

更新日期：2003-04-01 00:00:00

abstract：:N-Pyridinyl(methyl)-N1-substituted-3-indolepropanamides (17-32) were prepared starting from the corresponding acids and screened for their anti-inflammatory activity. Pharmacomodulation was carried out on the indole and amidic nitrogens by incorporation of substituents associated with higher potency in previously synt...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Gallard A,Duflos M,Nourrisson MR,Le Baut G,Grimaud N,Petit JY

更新日期：2003-04-01 00:00:00

abstract：:The synthesis and pharmacological evaluation of new 3-(imidazol-4(5)-ylmethylene)indolin-2-ones, analogues of SU-5416, are reported. The final compounds 20-51 were obtained by Knoevenagel coupling between the substituted indolin-2-ones 1-15 and either the formylimidazole derivatives 16-18 or 2-formyl-3,5-dimethylpyrro...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Braud E,Duflos M,Nourrisson MR,Tonnerre A,Picot C,Le Baut G,Renard P,Pfeiffer B,Tucker G

更新日期：2003-06-01 00:00:00

abstract：:Terephthalic acid based derivatives containing beta- and gamma-amino acid residues were prepared as antagonists of the leukocyte cell adhesion process that is mediated through the interaction of the very late antigen 4 (VLA-4) and the vascular cell adhesion molecule 1 (VCAM-1). The compounds 2, 10-12, 14, and 16-17 in...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Müller G,Albers M,Hessler G,Lehmann TE,Okigami H,Tajimi M,Bacon K,Rölle T

更新日期：2003-08-01 00:00:00

abstract：:The adenosine kinase inhibitory (AKI) activity of 5-iodo and diaryl analogues of tubercidin is quantitatively analyzed using Fujita-Ban and Hansch type analyses. The Fujita-Ban analysis being a non-parametric approach assigned the highest contribution to Cl at the X-position, C6H4-4-Cl, C6H5, 2-furanyl and I at the Y-...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Singh P,Kumar R,Sharma BK

更新日期：2003-10-01 00:00:00

abstract：:Curcumin, the major active component of the spice turmeric, is recognised as a safe compound with great potential for cancer chemoprevention and cancer therapy. It induces apoptosis, but its initiation mechanism remains poorly understood. Curcumin has been assessed on the human cancer cell lines, TK-10, MCF-7 and UACC...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Martín-Cordero C,López-Lázaro M,Gálvez M,Ayuso MJ

更新日期：2003-12-01 00:00:00

abstract：:The kinetics of heavy metal ions inhibition of jack bean urease was studied by progress curve analysis in a reaction system without enzyme-inhibitor preincubation. The inhibition was found to be biphasic with an initial, small inhibitory phase changing over the time course of 5-10 min into a final linear steady state ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Zaborska W,Krajewska B,Olech Z

更新日期：2004-02-01 00:00:00

abstract：:Bambuterol, a dimethylcarbamate, carbamoylates butyrylcholinesterase (BChE; EC 3.1.1.8). The carbamoylated enzyme is not very stable and the final product of the two-step hydrolysis is a bronchodilator drug, terbutaline (1-(3,5-dihydroxyphenyl)-2-t-butylamino-ethanol sulphate). Both bambuterol and terbutaline inhibit ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kovarik Z,Simeon-Rudolf V

更新日期：2004-04-01 00:00:00

abstract：:These ligands (L) show a bidentate behavior, forming octahedral ruthenium complexes. The title complexes were subjected to in-vivo anticancer activity tests against a transplantable murine tumor cell line, Ehrlich's Ascitic Carcinoma (EAC) and in-vitro antibacterial activity against several Gram positive and Gram nega...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Mazumder UK,Gupta M,Bhattacharya S,Karki SS,Rathinasamy S,Thangavel S

更新日期：2004-04-01 00:00:00

abstract：:Our previously developed approach to the development of QSAR equations for benzene derivatives, originally for phenylalkylamine hallucinogens, has been applied to four new systems: sulfonamide inhibitors of the enzymes carbonic anhydrase, thrombin, trypsin, and Clostridium histolyticum collagenase. The novel features ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Supuran CT,Clare BW

更新日期：2004-06-01 00:00:00

abstract：:A series of 1-(3-aryl-2-propenoyl)-4-oxopiperidines (1) as well as some related semicarbazones (2) and thiosemicarbazones (3) were prepared in order to determine whether the relative locations of aryl rings and amidic groups would lead to novel anticonvulsant agents. Initially the compounds were administered intraperi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Dimmock JR,Gunda SG,Vashishtha SC,Zello GA,Das U,Nienaber KH,Stables JP,Allen TM,Santos CL

更新日期：2004-08-01 00:00:00

abstract：:Dicoumarols 1-10 with substituted phenyl residues at C-11 were synthesized and screened for their urease inhibition effects. All synthesized compounds showed varying degree of urease inhibitory activity ranging from IC50 = 74.30-91.35 microM. ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Khan KM,Iqbal S,Lodhi MA,Maharvi GM,Perveen S,Choudhary MI,Atta-Ur-Rahman,Chohan ZH,Supuran CT

更新日期：2004-08-01 00:00:00

abstract：:Inhibition of Na+/K+-ATPase activity from human erythrocyte membranes and commercial porcine cerebral cortex by in vitro single and simultaneous exposure to digoxin and gitoxin was investigated to elucidate the difference in the mechanism of the enzyme inhibition by structurally different cardiac glycosides. The drugs...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Krstić D,Krinulović K,Spasojević-Tisma V,Joksić G,Momić T,Vasić V

更新日期：2004-10-01 00:00:00

abstract：:A series of 2',3'-didehydro-2',3'-dideoxynucleosides substituted with an alkynylhydroxy- (6, 7, 12 and 13) and alkynylamino- (20) groups at the C-5 position were synthesized. All these five target modified nucleosides were tested for anti-human immunodeficiency virus type 1 activity in CEM-SS and MT-4 cells and unfort...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ciurea A,Fossey C,Gavriliu D,Delbederi Z,Sugeac E,Laduree D,Schmidt S,Laumond G,Aubertin AM

更新日期：2004-12-01 00:00:00

abstract：:Diphenylamine-2,2'-dicarboxylic acid and its Cu(II), Ni(II), Co(II) and Zn(II) complexes have been synthesized and characterized by their elemental analyses, molecular weight determination, molar conductance, infrared and electronic spectra and magnetic measurements. The Zinc complex was tested by different methods fo...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Mohan G,Nagar R,Agarwal SC,Mehta KA,Rao CS

更新日期：2005-02-01 00:00:00

abstract：:A series of N-acyl peptides 1-9, containing an inhibitor of glucosamine-6-phosphate synthase have been synthesised and tested against Candida strains. N-Acylated peptides inhibit glucosamine-6-phosphate synthase in cell free extracts from Candida albicans. Antifungal activities of the tested compounds correlated with ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Andruszkiewicz R,Zieniawa T,Walkowiak A

更新日期：2005-04-01 00:00:00

abstract：:Beta-Alanine exhibits neurotransmitter activity and is a component of the anti-glycation agent carnosine. We propose that beta-alanine may have additional properties which may be of physiological significance. Interestingly, stress modulates the level of beta-alanine, which regulates excitotoxicity responses and preve...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Mehta AD,Seidler NW

更新日期：2005-04-01 00:00:00

abstract：:The ethanolic extract derived from aerial parts of an indigenous medicinal plant Paeonia emodi was screened for enzyme inhibition activities against Urease (jack bean and Bacillus pasteurii) and alpha-Chymotrypsin. The extract was also investigated for its radical scavenging activity using DPPH assay. The crude extrac...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Khan T,Ahmad M,Nisar M,Ahmad M,Lodhi MA,Choudhary MI

更新日期：2005-06-01 00:00:00

abstract：:The inhibition of xanthine oxidase (XO) activity by the purine analogue 6-(N-benzoylamino)purine was evaluated and compared with the standard inhibitor, allopurinol and the parent compound adenine. 6-(N-benzoylamino)purine is a highly potent inhibitor of XO (IC50 = 0.45 microM) and comparable to allopurinol (IC50 = 0....

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Tamta H,Thilagavathi R,Chakraborti AK,Mukhopadhyay AK

更新日期：2005-08-01 00:00:00

abstract：:The discovery of new topoisomerase I inhibitors is necessary since most of the antitumor drugs are targeted against type II and only a very few can specifically affect type I. Topoisomerase poisons generate toxic DNA damage by stabilization of the covalent DNA-topoisomerase cleavage complex and some have therapeutic e...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Gálvez M,Martín-Cordero C,Ayuso MJ

更新日期：2005-08-01 00:00:00

abstract：:Kinetics and inhibition of Na(+)/K(+)-ATPase and Mg(2+)-ATPase activity from rat synaptic plasma membrane (SPM), by separate and simultaneous exposure to transition (Cu(2+), Zn(2+), Fe(2+) and Co(2+)) and heavy metals (Hg(2+) and Pb(2+)) ions were studied. All investigated metals produced a larger maximum inhibition o...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Krstić D,Krinulović K,Vasić V

更新日期：2005-10-01 00:00:00

abstract：:Cibacron blue is a potent inhibitor of 3-HBA-6-hydroxylase at a concentration < 1 microM. Kinetic analyses revealed that at a concentration below 0.5 microM the dye behaves as an uncompetitive inhibitor with respect to 3-HBA and competes with NADH for the same site on the enzyme. The alteration of the near-UV CD spect...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Sumathi S,Dasgupta D

更新日期：2006-02-01 00:00:00

abstract：:Cadmium ion activates arginase from many species of organisms but is an inhibitor of arginase from many other species. The purpose of this study was to investigate the inhibition of rat liver and kidney arginase by cadmium ion. Rat kidney arginase was inhibited by much lower concentrations of cadmium ion than rat live...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Tormanen CD

更新日期：2006-02-01 00:00:00

abstract：:The results of Quantitative Structure-Activity Relationship (QSAR) analyses on three series of CYP3A4 inhibitors are reported for enzyme inhibition expressed as Ki values. These include a small series of structurally related statins and two larger groupings of structurally diverse compounds, some of which display comp...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Lewis DF,Lake BG,Dickins M

更新日期：2006-04-01 00:00:00