Synthesis and biological evaluation of novel 3-(quinolin-4-ylamino)benzenesulfonamidesAQ3 as carbonic anhydrase isoforms I and II inhibitors.

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：:Structure modification of the side chain of the lead compound benzoxanthone provided a series of benzoxanthone analogues and 12 of them were first reported. The results showed that most of these compounds had moderate cytotoxicity against tumour cells with the 50% inhibition concentration in the micromolar range. Furt...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Cheng P,Zhu L,Guo W,Liu W,Yao J,Dong G,Zhang Y,Zhuang C,Sheng C,Miao Z,Zhang W

更新日期：2012-06-01 00:00:00

abstract：:Exposure of the N-methoxycarbonyl-bicyclic-keto-acid 5 (improved preparation) to the Barnick beta-keto-acid synthesis yielded an aqueous solution of the sodium salts of the beta-keto-acids 26 and 27 which on heating at 60-65 degrees C furnished the N-methoxycarbonyl-tricyclic-ketone 9 (55%) plus the hydroxy-ketone 28 ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Bowman MA,Bowman RE,Davies RV,Haran G,Harris PJ,Smith HJ,Steele RW,Walker N,Whiting K

更新日期：2002-06-01 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：:The whole plants of Carpesium genus are used in traditional medicine as anti-pyretic, analgesic and vermifugic, including a topical application for sores and inflammation. A previous study on Carpesium genus suggested that the antiplasmodial activity against Plasmodium falciparum was due to the existence of 11(13)- de...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kim JJ,Chung IM,Jung JC,Kim MY,Moon HI

更新日期：2009-02-01 00:00:00

abstract：:In this study, the synthetic way to new N-pyridinyl(methyl)indolylpropanamides acting as non acidic NSAIDs has been described. Pharmacomodulation was carried out at N(1) and C(5) of the indole ring and at the level of the propanamide chain. N(3)-pyridinylmethyl-[1(4-chlorobenzyl-5-chloroindol-3-yl)propanamide represen...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Dassonville A,Lardic M,Breteche A,Nourrisson MR,Le Baut G,Grimaud N,Petit JY,Duflos M

更新日期：2008-10-01 00:00:00

abstract：:An economical and efficient one-pot synthesis of a series of novel 5-aryl-6-cinnamoyl-7-methyl-flavanones has been developed by simple refluxing of cinnamoyl chalcones with NaOAc in aqueous ethanol in quantitative yields. These flavanones were screened for their in vitro antioxidant and in vivo antidyslipidemic activi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Sharma A,Anand N,Sharma R,Chaturvedi U,Khanna AK,Bhatia G,Tripathi RP

更新日期：2012-04-01 00:00:00

abstract：:17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) is a key enzyme in the biosynthesis of 17β-estradiol. Novel estrone-based compounds bearing various 15β-oxa-linked substituents and hydroxy, methoxy, benzyloxy, and sulfamate groups in position C3 as potential 17β-HSD1 inhibitors have been synthesized. In addition, in...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Herman BE,Kiss A,Wölfling J,Mernyák E,Szécsi M,Schneider G

更新日期：2019-12-01 00:00:00

abstract：:Pyrogallol is found naturally in crops and fruits of many plants. It is also an active ingredient of many pharmaceuticals. For this reason, we employed different in vitro antioxidant assays such as cupric ion Cu(2+) reducing power, Fe(3+) reducing power, total antioxidant activity by ferric thiocyanate method, ABTS ra...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ozturk Sarikaya SB

更新日期：2015-01-01 00:00:00

abstract：:Chemotypes comprising the d-annulated 1,3-dihydro-2H-1-benzazepin-2-one scaffold derived from the paullone structure were found to be potent vascular endothelial growth factor receptor 2 (VEGF-R2) kinase inhibitors. Three-dimensional quantitative structure-activity relationship (3D-QSAR) and docking studies were perfo...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Lan P,Sun JR,Chen WN,Sun PH,Chen WM

更新日期：2011-06-01 00:00:00

abstract：:A series of 1,2,4-trisubstituted 5-imidazolinone derivatives were synthesized by Erlenmeyer condensation of benzoylglycine (hippuric acid) with different aldehydes in the presence of sodium acetate and acetic anhydride. The derivatives of the compounds were prepared by condensation of some known sulpha drugs with 5-ox...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Moorthy NS,Saxena V,Karthikeyan C,Trivedi P

更新日期：2012-04-01 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：:Poly(ADP-ribose) polymerase (PARP)-1 inhibitor has been suggested to attenuate the ischemia-reperfusion injury. We investigated the protective effect of the cardioplegia with a PARP-1 inhibitor, 4-hydoxyquinazoline (4-HQ), against myocardial ischemia-reperfusion injury. Isolated rat hearts were perfused on a Langendor...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Yamazaki K,Tanaka S,Sakata R,Miwa S,Oriyanhan W,Takaba K,Minakata K,Marui A,Ikeda T,Toyokuni S,Komeda M,Ueda K

更新日期：2013-02-01 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：:Matricaria chamomilla L. contains antioxidant flavonoids that can have their bioactivity enhanced by enzymatic hydrolysis of specific glycosyl groups. This study implements an untargeted metabolomics approach based on ultra-performance liquid chromatography coupled with electrospray ionisation quadrupole time-of-fligh...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Franco EPD,Contesini FJ,Lima da Silva B,Alves de Piloto Fernandes AM,Wielewski Leme C,Gonçalves Cirino JP,Bueno Campos PR,de Oliveira Carvalho P

更新日期：2020-12-01 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：:Synthesis and pharmacological evaluation of various 2-(4-isobutylphenyl)propanoic acid derivatives containing 1,3,4-thiadiazole and thiadiazolo[3,2-a][1,3,5]triazine-5-thione nucleus is reported here. The structures of new compounds are supported by IR, (1)H & (13)C NMR data. These compounds were tested in vivo for th...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Raval JP,Gandhi AN,Akhaja TN,Myangar KN,Patel NH

更新日期：2012-02-01 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：:Fatty acid synthase (FAS) has been proposed to be a new drug target for the development of anticancer agents because of the significant difference in expression of FAS between normal and tumour cells. Since a n-hexane-soluble extract from Ginkgo biloba was demonstrated to inhibit FAS activity in our preliminary test, ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Oh J,Hwang IH,Hong CE,Lyu SY,Na M

更新日期：2013-06-01 00:00:00

abstract：:Organophosphorus compounds pose a potential threat to both military and civilian populations. Since post-exposure therapy has its limitations, our research was focused on the possibility of improving pretreatment in order to limit the toxic effects of tabun. We determined the protective index of various combinations o...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Berend S,Katalinić M,Vrdoljak AL,Kovarik Z,Kuca K,Radić B

更新日期：2010-08-01 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：:The tyrosine kinase inhibitory action of the derivatives of N-Phenyl-N'-{4-(4-quinolyloxy)phenyl}urea is quantitatively analyzed using multiple regression analysis. The analysis has helped to ascertain the role of different substituents in explaining the observed inhibitory actions of these compounds for two receptors...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Sharma BK,Sharma SK,Singh P,Sharma S

更新日期：2008-04-01 00:00:00

abstract：:Carbonic anhydrases (CAs, EC 4.2.1.1) had six genetically distinct families described to date in various organisms. There are 16 known CA isoforms in humans. Human CA isoenzymes I and II (hCA I and hCA II) are ubiquitous cytosolic isoforms. Acetylcholine esterase (AChE. EC 3.1.1.7) is a hydrolase that hydrolyzes the n...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Taslimi P,Gulcin I,Ozgeris B,Goksu S,Tumer F,Alwasel SH,Supuran CT

更新日期：2016-01-01 00:00:00

abstract：:New, except 1d, melatonin analogue benzimidazole derivatives were synthesized and characterized in the present study. The potential role of melatonin as an antioxidant by scavenging and detoxifying ROS raised the possibility that compounds that are analogous to melatonin can also be used for their antioxidant properti...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Gurer-Orhan H,Orhan H,Suzen S,Püsküllü MO,Buyukbingol E

更新日期：2006-04-01 00:00:00

abstract：:In a new group of 3-methyl-2-phenyl-1-substituted-indole derivatives (10a-f), the indomethacin analogs were prepared via the Fisher indole synthesis reaction of propiophenone with appropriately substituted phenylhydrazine hydrochloride. This is followed by the insertion of the appropriate benzyl or benzoyl fragment. A...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Abdellatif KR,Lamie PF,Omar HA

更新日期：2016-01-01 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：: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：: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：:To develop multifunctional aldose reductase (AKR1B1) inhibitors for anti-diabetic complications, a novel series of 2-phenoxypyrido[3,2-b]pyrazin-3(4H)-one derivatives were designed and synthesised. Most of the derivatives were found to be potent and selective against AKR1B1, and 2-(7-chloro-2-(3,5-dihydroxyphenoxy)-3-...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Hao X,Qi G,Ma H,Zhu C,Han Z

更新日期：2019-12-01 00:00:00

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