Synthesis, characterization, and antimicrobial evaluation of some new hydrazinecarbothioamide, 1,2,4-triazole and 1,3,4-thiadiazole derivatives.

abstract：:The limited arsenal of synthetic antifungal agents and the emergence of resistant Candida strains have prompted the researchers towards the investigation of naturally occurring compounds or their semisynthetic derivatives in order to propose new innovative hit compounds or new antifungal combinations endowed with redu...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Carradori S,Chimenti P,Fazzari M,Granese A,Angiolella L

更新日期：2016-01-01 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：: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：: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：: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：: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：:Resveratrol is a natural polyphenol with plethora of biological activities. Resveratrol has previously shown to decrease DNA-methyltransferase (DNMT) enzymes expression and to reactivate silenced tumor suppressor genes. Currently, it seems that no resveratrol analogs have been developed as DNMT inhibitors. Recently, w...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Aldawsari FS,Aguayo-Ortiz R,Kapilashrami K,Yoo J,Luo M,Medina-Franco JL,Velázquez-Martínez CA

更新日期：2016-10-01 00:00:00

abstract：:Human inosine 5'-monophosphate dehydrogenase 2 (hIMPDH2), being an age-old target, has attracted attention recently for anticancer drug development. Mycophenolic acid (MPA), a well-known immunosuppressant drug, was used a lead structure to design and develop modestly potent and selective analogues. The steep structure...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Shah CP,Kharkar PS

更新日期：2018-12-01 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：:Phthalates, used in medical devices (MDs), have been identified as reproductive and developmental toxicants. Their toxicity varies somewhat depending on the specific phthalate and is in part linked to the activation of Peroxisome Proliferating-Activated Receptors (PPARs). So, the use of MDs containing targeted phthala...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kambia N,Farce A,Belarbi K,Gressier B,Luyckx M,Chavatte P,Dine T

更新日期：2016-01-01 00:00:00

abstract：:HGF/c-Met signalling pathway plays an important role in the development of cancers. A series of 6,7-dimethoxy-4-anilinoquinolines possessing benzimidazole moiety were synthesised and identified as potent inhibitors of the tyrosine kinase c-Met. Their in vitro biological activities against three cancer cell lines (A549...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Zhang QW,Ye ZD,Shen C,Tie HX,Wang L,Shi L

更新日期：2019-12-01 00:00:00

abstract：:A novel set of 16 hybrids of bromopyrrole alkaloids with aroyl hydrazone were designed, synthesized and evaluated for antibacterial and antibiofilm activities against methicillin-resistant Staphylococcus aureus (MRSA; ATCC 43866), methicillin-susceptible Staphylococcus aureus (MSSA; ATCC 35556) and Staphylococcus epid...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Rane RA,Sahu NU,Shah CP,Shah NK

更新日期：2014-06-01 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：: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：:Thirty new aryl-pyridazinone-substituted benzenesulphonylurea derivatives (I-XXX) were synthesized and evaluated for their anti-hyperglycaemic activity in glucose-fed hyperglycaemic normal rats. Twenty-three compounds (III-XI, XIV-XVII, XIX-XXIV, XXVI and XXVIII-XXX) showed more or comparable area under the curve (AUC...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Yaseen R,Pushpalatha H,Reddy GB,Ismael A,Ahmed A,Dheyaa A,Ovais S,Rathore P,Samim M,Akthar M,Sharma K,Shafi S,Singh S,Javed K

更新日期：2016-12-01 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：:[60]Fullerene-peptides represent a simple yet chemically diverse example of a bio-nano conjugate. The C60 moiety provides the following attributes to the conjugate: (a) precise three-dimensional architecture, (b) a large hydrophobic mass and (c) unique electronic properties. Conversely, the peptide component provides:...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Barron AR

更新日期：2016-01-01 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：:Flavonoids, polyphenolic phytochemicals, are ubiquitous in plants and are commonly present in the human diet. They may exert diverse beneficial effects, including antioxidant and anticarcinogenic activities. The present study was designed to evaluate three biomolecules that play important roles in the apoptotic proces...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： de Sousa RR,Queiroz KC,Souza AC,Gurgueira SA,Augusto AC,Miranda MA,Peppelenbosch MP,Ferreira CV,Aoyama H

更新日期：2007-08-01 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：: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：: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：:The inhibition of neuraminidase from Clostridium chauvoei (jakari strain) with partially purified methanolic extracts of some plants used in Ethnopharmacological practice was evaluated. Extracts of two medicinal plants, Tamarindus indicus and Combretum fragrans at 100-1000 microg/ml, both significantly reduced the act...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Useh NM,Nok AJ,Ambali SF,Esievo KA

更新日期：2004-08-01 00:00:00

abstract：:The reactivity of [1,2,3]triazolo[1,5-a]pyridines 1 is described. Triazolopyridines react with electrophiles in two contrasting ways, giving 3-substituted triazolopyridines 2, or products 3, resulting from triazolo ring opening with loss of molecular nitrogen. The triazolopyridines can be lithiated at -40 degrees C by...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Abarca-González B

更新日期：2002-12-01 00:00:00

abstract：:This work has been focused on testing the influence of two selected Pt(II) complexes cisplatin, Pt(NH₃)₂Cl₂, and [Pt(dach)Cl₂] on the activity of porcine pancreatic phospholipase A₂ (PLA₂). It has been assumed that this enzyme plays a role in carcinogenesis and that it could be a target in the tumour therapy. The resu...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Radisavljević M,Kamčeva T,Bugarčić ŽD,Petković M

更新日期：2013-08-01 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：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：UNLABELLED:Context: Garcinia hombroniana Pierre, known as manggis hutan in Malaysia is a rich source of xanthones and benzophenones. OBJECTIVES:This study was aimed to isolate and characterize potential cholinesterase inhibitors from the extracts of G. hombroniana bark and investigate their interactions with the enzym...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Jamila N,Khairuddean M,Yeong KK,Osman H,Murugaiyah V

更新日期：2015-02-01 00:00:00

abstract：:Selective PDE3 inhibitors improve cardiac contractility and may be used in congestive heart failure. However, their proarrhythmic potential is the most important side effect. In this research we designed, synthesized and evaluated the potential cardiotonic activity of thirteen PDE3 inhibitors (4-[(4-methyl-2-oxo-1,2-d...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Sadeghian H,Seyedi SM,Saberi MR,Nick RS,Hosseini A,Bakavoli M,Mansouri SM,Parsaee H

更新日期：2009-08-01 00:00:00

abstract：:The inhibition effect of metal ions on beta amylase activity was studied. The inhibitor-binding constant (Ki) was determined by spectrophotometric and isothermal titration calorimetric (ITC) methods. The binding of calcium, magnesium and zinc ion as inhibitors at the active site of barley beta amylase was studied at p...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Dahot MU,Saboury AA,Moosavi-Movahedi AA

更新日期：2004-04-01 00:00:00