Synthesis, activity and mechanism of alkoxy-, carbamato-, sulfonamido-, thioureido-, and ureido-derivatives of 2,4,5-trimethylpyridin-3-ol against inflammatory bowel disease.

abstract：:The synthesis of new 4-[2-(alkylamino)ethylthio]pyrrolo[1,2-a]quinoxaline derivatives la-1 is described in five or six steps starting from various substituted nitroanilines 2a-e. The bioisostere 5-[2-(alkylamino)ethylthio]pyrrolo[1,2- a]thieno[3,2-e]pyrazine 1m was also prepared. The new derivatives were evaluated as ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Vidaillac C,Guillon J,Moreau S,Arpin C,Lagardère A,Larrouture S,Dallemagne P,Caignard DH,Quentin C,Jarry C

更新日期：2007-10-01 00:00:00

abstract：:Tetrahydrocannabinol and other mixed cannabinoid (CB) receptors CB(1)/CB(2) receptor agonists are well established to elicit antinociceptive effects and psychomimetic actions, however, their potential for abuse have dampened enthusiasm for their therapeutic development. In an effort to refine a semi-rigid structural f...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Taher AT,Kadry HH,Allarà M,Di Marzo V,Abadi AH,Abouzid KA

更新日期：2013-06-01 00:00:00

abstract：:Lipopeptides have been reported to exhibit anti-obesity effects. In this study, we obtained a Bacillus velezensis strain FJAT-52631 that could coproduce iturins, fengycins, and surfactins. Results showed that the FJAT-52631 crude lipopeptide, purified fengycin, iturin, and surfactin standards exhibited strong inhibiti...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Chen MC,Liu TT,Wang JP,Chen YP,Chen QX,Zhu YJ,Liu B

更新日期：2020-12-01 00:00:00

abstract：:The synthesis and antioxidant evaluation of some novel benzimidazole derivatives (10-24) are described. Antioxidant properties of the compounds were investigated employing various in vitro systems viz., microsomal NADPH-dependent inhibition of lipid peroxidation (LP), interaction of 2,2-diphenyl-1-picrylhydrazyl (DPPH...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ayhan-Kilcigil G,Kuş C,Coban T,Can-Eke B,Ozbey S,Iscan M

更新日期：2005-10-01 00:00:00

abstract：:Lignostilbene-alpha,beta-dioxygenase (LSD, EC 1.13.11.43) is involved in oxidative cleavage of the central double bond of lignostilbene to form the corresponding aldehydes by a mechanism similar to those of 9-cis-epoxycarotenoid dioxygenase and beta-carotene 15,15'-dioxygenase, key enzymes in abscisic acid biosynthesi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Han SY,Inoue H,Terada T,Kamoda S,Saburi Y,Sekimata K,Saito T,Kobayashi M,Shinozaki K,Yoshida S,Asami T

更新日期：2003-06-01 00:00:00

abstract：:A series of quinazoline derivatives with benzylidene hydrazine carboxamide were designed and synthesised as EGFR inhibitors. Most compounds exhibited exceptional anti-proliferative activity against A549, HepG2, MCF-7 and H1975 cells. Furthermore, six compounds demonstrated excellent inhibition activity against EGFRWT ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Wang C,Xu S,Peng L,Zhang B,Zhang H,Hu Y,Zheng P,Zhu W

更新日期：2019-12-01 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：: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：:Three series of 5-bromo-thieno[2,3-b]pyridines bearing amide or benzoyl groups at position 2 were prepared as pim-1 inhibitors. All the prepared compounds were tested for their pim-1 enzyme inhibitory activity. Two compounds (3c and 5b) showed moderate pim-1 inhibitory activity with IC50 of 35.7 and 12.71 μM, respecti...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Naguib BH,El-Nassan HB

更新日期：2016-12-01 00:00:00

abstract：:Previously, a glycoglycerolipid isolated from marine algae was reported to be a potent and selective inhibitor of the human Myt1 kinase, an enzyme involved in cell cycle regulation with great potential as an anti-cancer target. Based on that report, a lot of research effort has been invested by several working groups ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Rohe A,Göllner C,Erdmann F,Sippl W,Schmidt M

更新日期：2015-06-01 00:00:00

abstract：:Twenty-five new N-[4-(benzothiazole-2-yl)phenyl]acetamide derivatives bearing different heterocyclic ring systems were synthesized using 2-(4-aminophenyl)benzothiazole structure as a pharmacophoric group. Final compounds were screened for their potential antitumor activity in vitro against approximately 60 human tumor...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Yurttaş L,Tay F,Demirayak Ş

更新日期：2015-06-01 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：:The two β-carbonic anhydrases (CAs, EC 4.2.1.1) recently cloned and purified from the ascomycete fungus Sordaria macrospora, CAS1 and CAS2, were investigated for their inhibition with a panel of 39 aromatic, heterocyclic, and aliphatic sulfonamides and one sulfamate, many of which are clinically used agents. CAS1 was ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Vullo D,Lehneck R,Pöggeler S,Supuran CT

更新日期：2018-12-01 00:00:00

abstract：:Nerve agents such as sarin, cyclosarin and tabun are organophosphorus substances able to inhibit the enzyme acetylcholinesterase (AChE; EC 3.1.1.7). AChE reactivators and anticholinergics are generally used as antidotes in the case of intoxication with these agents. None of the known AChE reactivators is able to react...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Hrabinova M,Musilek K,Jun D,Kuca K

更新日期：2006-10-01 00:00:00

abstract：:Serum paraoxonase (PON1) is a high-density lipoprotein (HDL)-associated enzyme that protects lipoproteins, both low-density lipoprotein (LDL) and HDL, against oxidation, and is considered as an antioxidative/anti-inflammatory component of HDL. In this study, PON1 was purified from bovine serum by ammonium sulfate prec...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Sayın M,Guler OO

更新日期：2015-02-01 00:00:00

abstract：:A revisited synthesis of 2-aryl-6-methyl-1,2-dihydro-1H-pyridin-4-ones and their saturated analogues 2-aryl-6-methylpiperidin-4-ols is described. A five steps procedure, using the sulfinimine chemistry, to prepare a key intermediate beta-(6-chloronicotinic)-beta-amino ester is also reported. In vivo spontaneous workin...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Leflemme N,Freret T,Boulouard M,Dallemagne P,Rault S

更新日期：2005-12-01 00:00:00

abstract：:A series of novel benzene sulfonamides (previously evaluated as selective cyclooxygenase-2 inhibitors) has been profiled against human carbonic anhydrases I, II, IV and VII in an attempt to observe the manifestation of the well established "tail" approach for designing potent, isoform-selective inhibitors of carbonic ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Supuran CT,Kalinin S,Tanç M,Sarnpitak P,Mujumdar P,Poulsen SA,Krasavin M

更新日期：2016-01-01 00:00:00

abstract：:A small library of phosphorylated sulfamates (N-(O-alkylsulfamoyl)-phosphoramidic acids) incorporating long aliphatic chains (C8-C16) has been synthesized and investigated for their interaction with two physiologically relevant carbonic anhydrase (CA) isozymes. These compounds behaved as very potent inhibitors of both...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Bonnac L,Innocenti A,Winum JY,Casini A,Montero JL,Scozzafava A,Barragan V,Supuran CT

更新日期：2004-06-01 00:00:00

abstract：:Seven triterpenoid saponins were identified in methanolic extracts of seeds of the Zolfino bean landrace (Phaseolus vulgaris L.) by HPLC fractionation, revealing their ability to inhibit highly purified human recombinant aldose reductase (hAKR1B1). Six of these compounds were associated by MS analysis with the followi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Balestri F,De Leo M,Sorce C,Cappiello M,Quattrini L,Moschini R,Pineschi C,Braca A,La Motta C,Da Settimo F,Del-Corso A,Mura U

更新日期：2019-12-01 00:00:00

abstract：:Trypanothione reductase (TR) is a major enzyme in trypanosomatids. Its substrate, trypanothione is a molecule containing a tripeptide (L-glutamic acid-cysteine-glycine) coupled to a polyamine, spermidine. This redox system (TR/Trypanothione) is vital for parasite survival within the host cell and has been described as...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Castro-Pinto DB,Lima EL,Cunha AS,Genestra M,De Léo RM,Monteiro F,Leon LL

更新日期：2007-02-01 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 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：:Two fractions of rat intestinal alkaline phosphatase (IAP) were detected by Western blot: 168 +/- 6 and 475 +/- 45 kDa. The low molecular weight fraction constitutes 43% of the isolated proteins exhibiting 82% of the enzymatic activity, and a heavier fraction constitutes 57% of the isolated proteins and has 18% of the...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Brun LR,Brance ML,Rigalli A,Puche RC

更新日期：2006-12-01 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：:A series of hydroxylic compounds (1-10, NK-154 and NK-168) have been assayed for the inhibition of three physiologically relevant carbonic anhydrase isozymes, the cytosolic isozymes I, II and tumor-associated isozyme IX. The investigated compounds showed inhibition constants in the range of 0.068-4003, 0.012-9.9 and 0...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Durdagi S,Korkmaz N,Işık S,Vullo D,Astley D,Ekinci D,Salmas RE,Senturk M,Supuran CT

更新日期：2016-12-01 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：:Carbonic anhydrases (CAs, EC 4.2.1.1) are crucial metalloenzymes that are involved in diverse bioprocesses. We report the synthesis and biological evaluation of novel series of benzenesulfonamides incorporating un/substituted ethyl quinoline-3-carboxylate moieties. The newly synthesised compounds were in vitro evaluat...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Al-Sanea MM,Elkamhawy A,Paik S,Bua S,Ha Lee S,Abdelgawad MA,Roh EJ,Eldehna WM,Supuran CT

更新日期：2019-12-01 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：: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：: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