In vivo experimental approach to treatment against tabun poisoning.

abstract：:Novel 6-substituted thiazolocarbazole derivatives have been synthesized under microwave irradiation via the corresponding imino-1,2,3-dithiazoles. In vitro antitumor potential of these polyheterocyclic compounds was evaluated. Among all the tested thiazolocarbazoles, compound 10 is the most effective in inhibiting cel...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Testard A,Picot L,Fruitier-Arnaudin I,Piot JM,Chabane H,Domon L,Thiery V,Besson T

更新日期：2004-12-01 00:00:00

abstract：:Coumarin, a naturally occurring or synthesised phytochemical, displays a wide range of biological activities. However, chromen-2-ones fused with 1,3-benzoxazine rings is not well documented and there is a gap in the literature which required engaging. The substituted-2-thioxo-chromen-oxazine linear compounds 14a-i and...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Morrison R,Al-Rawi JM

更新日期：2016-01-01 00:00:00

abstract：:C3 and C4 plant carbonic anhydrases (CAs) are zinc-enzymes that catalyze the reversible hydration of CO2. They are sub-divided in three classes: α, β and γ, being distributed between both photosynthetic subtypes. The C4 dicotyledon species Flaveria bidentis (L.) "Kuntze" contains a small gene family encoding three dis...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Dathan NA,Alterio V,Troiano E,Vullo D,Ludwig M,De Simone G,Supuran CT,Monti SM

更新日期：2014-08-01 00:00:00

abstract：UNLABELLED:Abstract In biological systems, the Keap1/Nrf2/antioxidant response element pathway determines the ability of mammalian cells to adapt and survive conditions of oxidative, electrophilic and inflammatory stress by regulating the production of cytoprotective enzymes NAD(P)H:quinone oxidoreductase 1 (NQO1, EC ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ghorab MM,Higgins M,Alsaid MS,Arafa RK,Shahat AA,Dinkova-Kostova AT

更新日期：2014-12-01 00:00:00

abstract：:Carbonic anhydrases (CAs) are widespread metalloenzymes in higher vertebrates including humans. A series of phenolic compounds, including guaiacol, 4-methylguaiacol, 4-propylguaiacol, eugenol, isoeugenol, vanillin, syringaldehyde, catechol, 3-methyl catechol, 4-methyl catechol and 3-methoxy catechol were investigated ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Scozzafava A,Passaponti M,Supuran CT,Gülçin İ

更新日期：2015-01-01 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：:Protein phosphatases are signalling molecules that regulate a variety of fundamental cellular processes including cell growth, metabolism and apoptosis. The aim of this work was to correlate the cytotoxicity of pervanadate and okadaic acid on HL60 cells and their effect on the phosphatase obtained from these cells. Th...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Freire AC,Aoyama H,Haun M,Ferreira CV

更新日期：2003-10-01 00:00:00

abstract：:Reaction of thiophosgene with 4-aminomethyl-benzenesulfonamide afforded 4-isothiocyanatomethyl-benzenesulfonamide, which by reaction with amines, amino acids and oligopeptides, lead to a series of new sulfonamides incorporating a 4-sulfamoylphenylmethylthiourea scaffold. These new thioureas showed strong affinities to...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Casini A,Scozzafava A,Mincione F,Menabuoni L,Supuran CT

更新日期：2002-10-01 00:00:00

abstract：:We describe herein the design, multicomponent synthesis and biological studies of new donepezil + chromone + melatonin hybrids as potential agents for Alzheimer's disease (AD) therapy. We have identified compound 14n as promising multitarget small molecule showing strong BuChE inhibition (IC50 = 11.90 ± 0.05 nM), mode...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Pachón-Angona I,Refouvelet B,Andrýs R,Martin H,Luzet V,Iriepa I,Moraleda I,Diez-Iriepa D,Oset-Gasque MJ,Marco-Contelles J,Musilek K,Ismaili L

更新日期：2019-12-01 00:00:00

abstract：:For the development of potent novel antileishmanial agents, 3,3'-(arylmethylene)bis(2-hydroxynaphthalene-1,4 dione) derivatives were synthesized from lawsone and evaluated for cytotoxicity on Leishmania donovani promastigotes as well as on leishmanial DNA topoisomerase-I. Enzyme inhibition studies were conducted with ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Sharma G,Chowdhury S,Sinha S,Majumder HK,Kumar SV

更新日期：2014-04-01 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 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：: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 Co(II), Ni(II) and Cu(II) complexes have been synthesized by template condensation of 2,6-diformyl-4-methylphenol and 3-substituted-4-amino-5-hydrazino-1,2,4-triazole with CoCl(2).6H(2)O, NiCl(2).6H(2)O and CuCl(2).2H(2)O chlorides in 2 + 2+2 molar ratio in ethanol. These complexes were characterized by el...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Avaji PG,Patil SA

更新日期：2009-02-01 00:00:00

abstract：:In this work, we reported the synthesis and evaluation of antibacterial and antifungal activities of three new compound series obtained from 6-(phenyl/4-chlorophenyl)imidazo[2,1-b]thiazole-3-acetic acid hydrazide: 2-{[6-(phenyl/4-chlorophenyl)imidazo[2,1-b]thiazol-3-yl]acetyl}-N-alkyl/arylhydrazinecarbothioamides (2a-...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Güzeldemirci NU,Satana D,Küçükbasmacı O

更新日期：2013-10-01 00:00:00

abstract：:In mammalian skin, melanocyte proliferation and melanogenesis can be stimulated by keratinocytes, fibroblasts and other regulatory factors. To determine whether hydroxybenzyl alcohols (HBAs) show more inhibitory in melanocytes cultured alone or in melanocytes co-cultured with keratinocytes, we developed a murine melan...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Liu SH,Chu IM,Pan IH

更新日期：2008-08-01 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：:Identification of a new class of antitumor agent capable to induce apoptosis without triggering necrotic cell death event is challenging. The present communication describes the multicomponent synthesis of seven new (1S,4S)-2,5-diazabicyclo[2.2.1]heptane-dithiocarbamates and their in vitro antiproliferative activity o...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Laskar S,Sánchez-Sánchez L,López-Ortiz M,López-Muñoz H,Escobar-Sánchez ML,Sánchez AT,Regla I

更新日期：2017-12-01 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：: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：: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：:3,6-Diazaphenothiazines were obtained in cyclization of 3-amino-3'-nitro-2,4'-dipyridinyl sulfide and the reaction of sodium 3-amino-2-pyridinethiolate with 4-chloro-3-nitropyridine followed by alkylation and heteroarylation. The thiazine ring formation ran via the Smiles rearrangement. The structure elucidation was b...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Morak-Młodawska B,Pluta K,Latocha M,Suwińska K,Jeleń M,Kuśmierz D

更新日期：2016-12-01 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：: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：:A large number of novel secondary sulfonamides based on the open saccharin scaffold were synthesized and evaluated as selective inhibitors of four different isoforms of human carbonic anhydrase (hCA I, II, IX and XII, EC 4.2.1.1). They were obtained by reductive ring opening of the newly synthesized N-alkylated saccha...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： D'Ascenzio M,Guglielmi P,Carradori S,Secci D,Florio R,Mollica A,Ceruso M,Akdemir A,Sobolev AP,Supuran CT

更新日期：2017-12-01 00:00:00

abstract：:Several (thiazol-2-yl)hydrazone derivatives from 2-, 3- and 4-acetylpyridine were synthesized and tested against human monoamine oxidase (hMAO) A and B enzymes. Most of them had an inhibitory effect in the low micromolar/high nanomolar range, being derivatives of 4-acetylpyridine selective hMAO-B inhibitors also at lo...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： D'Ascenzio M,Chimenti P,Gidaro MC,De Monte C,De Vita D,Granese A,Scipione L,Di Santo R,Costa G,Alcaro S,Yáñez M,Carradori S

更新日期：2015-12-01 00:00:00

abstract：:Melatonin (N-acetyl-5-methoxytryptamine) is the chief secretory product of the pineal gland and synthesized enzymatically from serotonin (5-hydroxytryptamine). These indoleamine derivatives play an important role in the prevention of oxidative damage. In the present study, DMPD radical scavenging and cupric ion (Cu(2+...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Gulçin I

更新日期：2008-12-01 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：:In this study, firstly, antioxidant and polyphenol oxidase (PPO) properties of Yomra apple were investigated. Seventeen phenolic constituents were measured by reverse phase-high-performance liquid chromatography (RP-HPLC). Total phenolic compounds (TPCs), ferric reducing antioxidant power (FRAP) and 2, 2-diphenyl-1-pi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Can Z,Dincer B,Sahin H,Baltas N,Yildiz O,Kolayli S

更新日期：2014-12-01 00:00:00

abstract：:An efficient and economical synthesis of some new fluorine substituted phthalides was accomplished from two γ-keto acids, 2-(4-fluorobenzoyl)benzoic acid and 2-(3,5-dinitro-4-flurobenzoyl)benzoic acid. Each acid was reacted with various phenolic compounds in presence of catalytic quantity of concentrated sulphuric aci...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Chamoli T,Rawat MS,Jacob M

更新日期：2012-10-01 00:00:00