Studies on synthetic and structural characterization of new fluorine substituted phthalides of pharmaceutical interest.

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 acid to get the phthalides. The structures of the synthesized compounds were established on the basis of their elemental analysis, spectral data and chemical reactions. Some of the synthesized phthalides exhibited antibacterial and antifungal activity on antimicrobial screening against human pathogenic bacteria and fungi.

authors

Chamoli T,Rawat MS,Jacob M

doi

10.3109/14756366.2011.606622

subject

Has Abstract

pub_date

2012-10-01 00:00:00

pages

748-57

issue

5

eissn

1475-6366

issn

1475-6374

journal_volume

27

pub_type

杂志文章
  • Design, synthesis and antistaphylococcal activity of marine pyrrole alkaloid derivatives.

    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

    pub_type: 杂志文章

    doi:10.3109/14756366.2013.793183

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

    更新日期:2014-06-01 00:00:00

  • 2-styrylchromones as novel inhibitors of xanthine oxidase. A structure-activity study.

    abstract::The purpose of this study was the evaluation of the xanthine oxidase (XO) inhibition produced by some synthetic 2-styrylchromones. Ten polyhydroxylated derivatives with several substitution patterns were synthesised, and these and a positive control, allopurinol, were tested for their effects on XO activity by measuri...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756360290019944

    authors: Fernandes E,Carvalho F,Silva AM,Santos CM,Pinto DC,Cavaleiro JA,Bastos Mde L

    更新日期:2002-02-01 00:00:00

  • Equations of substrate-inhibition kinetics applied to pig kidney diamine oxidase (DAO, E.C. 1.4.3.6).

    abstract::Pig kidney diamine oxidase (DAO) and other semicarbazide-sensitive amine oxidases (SSAO) show clear substrate-inhibition kinetics and a reaction-scheme mechanism based on two substrate binding sites. We evaluated several reaction scheme mechanisms with a non-linear regression program (NCSS), estimating R2, the constan...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756360310001605543

    authors: Ignesti G

    更新日期:2003-12-01 00:00:00

  • Luteolin downregulates IL-1β-induced MMP-9 and -13 expressions in osteoblasts via inhibition of ERK signalling pathway.

    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

    pub_type: 杂志文章

    doi:10.3109/14756366.2011.587415

    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

  • Resorcinol-, catechol- and saligenin-based bronchodilating β2-agonists as inhibitors of human cholinesterase activity.

    abstract::We investigated the influence of bronchodilating β2-agonists on the activity of human acetylcholinesterase (AChE) and usual, atypical and fluoride-resistant butyrylcholinesterase (BChE). We determined the inhibition potency of racemate and enantiomers of fenoterol as a resorcinol derivative, isoetharine and epinephrin...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2017.1326109

    authors: Bosak A,Knežević A,Gazić Smilović I,Šinko G,Kovarik Z

    更新日期:2017-12-01 00:00:00

  • Inhibitory effect of cisplatin and [Pt(dach)Cl2] on the activity of phospholipase A2.

    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

    pub_type: 杂志文章

    doi:10.3109/14756366.2012.666539

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

    更新日期:2013-08-01 00:00:00

  • Quantitative insights towards the design of potent deazaxanthine antagonists of adenosine 2B receptors.

    abstract::Adenosine receptors have been considered as potential targets for drug development, but one of the main obstacles to this goal is to selectively inhibit one receptor subtype over the others. This subject is particularly crucial for adenosine A2b receptor antagonists (AdoRA2B). The structure–activity relationships of x...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.3109/14756366.2013.830113

    authors: Paz OS,Brito CC,Castilho MS

    更新日期:2014-08-01 00:00:00

  • Synthesis of azatricyclodiones & octahydro-benzo[f]isoindoles and their antimicrobial evaluation.

    abstract::A series of azatricyclodiones and octahydro-benzo[f]isoindoles have been synthesized by (4+2) Diels-Alder cycloaddition of maleimides with furfuryl amine. Reaction of azatricyclodiones with isocyanates led to the respective ureides. All of the compounds were screened against a number of bacteria and fungi. One of the ...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756360701709383

    authors: Saxena N,Singh NT,Mishra M,Keshava GB,Shukla PK,Tripathi RP

    更新日期:2008-08-01 00:00:00

  • Synthesis and biological evaluation of new 3(2H)-pyridazinone derivatives as non-toxic anti-proliferative compounds against human colon carcinoma HCT116 cells.

    abstract::Novel 3(2H)-pyridazinone derivatives were designed, synthesised in satisfactory yields and evaluated in different experimental assays to assess their preliminary toxicity in vivo and anti-proliferative effects against HCT116 cell lines in vitro. Artemia salina lethality test provided LC50 values >100 µg/mL for all com...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2020.1755670

    authors: Özdemir Z,Utku S,Mathew B,Carradori S,Orlando G,Di Simone S,Alagöz MA,Özçelik AB,Uysal M,Ferrante C

    更新日期:2020-12-01 00:00:00

  • Ranitidine induces inhibition and structural changes in sucrase.

    abstract::Ranitidine is an antagonist of histamine-2 (H(2)) receptor. It is employed to treat peptic ulcer and other conditions in which gastric acidity must be reduced. Sucrase is a hydrolytic enzyme that catalyzes the breakdown of sucrose to its monomer content. A liquid of yeast sucrase was developed for treatment of congeni...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.3109/14756366.2011.601414

    authors: Minai-Tehrani D,Ghaffari M,Sobhani-Damavandifar Z,Minoui S,Alavi S,Osmani R,Ahmadi S

    更新日期:2012-08-01 00:00:00

  • Synthesis of new 8(S)-HETE analogs and their biological evaluation as activators of the PPAR nuclear receptors.

    abstract::Structural modifications around 8-HETE (8-hydroxyeicosatetraenoic acid), a natural agonist of the PPAR (peroxisome proliferator-activated receptor) nuclear receptors have led previously to the identification of a promising analog, the quinoline S 70655. Series of novel quinoline or benzoquinoline derivatives were desi...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.3109/14756360903468171

    authors: Liutkus M,Caijo F,Girard AL,Ayral E,Audinot V,Boutin JA,Renard P,Caignard DH,Dacquet C,Ktorza A,Mosset P,Grée R

    更新日期:2010-10-01 00:00:00

  • New natural urease inhibitors from Ranunculus repens.

    abstract::Phytochemical investigations on the chloroform and ethyl acetate soluble fractions of the roots of Ranunculus repens led to the isolation of methyl 3,4,5-trihydroxybenzoate 1, R(+)- 4-methoxydalbergione 2 and R(+)-dalbergiophenol 3. The structures of these compounds were established through spectral studies including ...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756360500319210

    authors: Khan WN,Lodhi MA,Ali I,Azhar-Ul-Haq,Malik A,Bilal S,Gul R,Choudhary MI

    更新日期:2006-02-01 00:00:00

  • Prediction of caspase-3 inhibitory activity of 1,3-dioxo-4-methyl-2,3-dihydro-1h-pyrrolo[3,4-c] quinolines: QSAR study.

    abstract::Neurodegenerative disorders are consequences of progressive and irreversible loss of neurons due to unwanted apoptosis which involves caspases, a group of cysteine proteases that cleave other proteins and inactivate them. Among several different groups of caspase enzymes, caspases-3 plays a key role in apoptosis and a...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756360701652476

    authors: Sharma S,Ravichandran V,Jain PK,Mourya VK,Agrawal RK

    更新日期:2008-06-01 00:00:00

  • Lipophilicity relationships in inhibitors of CYP2C9 and CYP2C19 enzymes.

    abstract::Quantitative structure-activity relationships (QSARs) within a series of cytochrome P450 2C9 (CYP2C9) and cytochrome P450 2C19 (CYP2C19) inhibitors are reported. In particular, it is noted that compound lipophilicity, in the form of log P values (where P is the octanol/water partition coefficient), is an important fac...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756360600703313

    authors: Lewis DF,Lake BG,Ito Y,Dickins M

    更新日期:2006-08-01 00:00:00

  • Quinazoline-urea, new protein kinase inhibitors in treatment of prostate cancer.

    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

    pub_type: 杂志文章

    doi:10.3109/14756360903169485

    authors: Garofalo A,Goossens L,Lemoine A,Farce A,Arlot Y,Depreux P

    更新日期:2010-04-01 00:00:00

  • Targeting human DNA polymerase alpha for the inhibition of keratinocyte proliferation. Part 1. Homology model, active site architecture and ligand binding.

    abstract::In order to understand the binding modes of human DNA polymerase alpha (pol alpha) inhibitors on a molecular level, a 3D homology model of the active site of the enzyme was proposed based on the application of molecular modelling methods and molecular dynamic simulations using available crystal coordinates of pol alph...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756360701433414

    authors: Richartz A,Höltje M,Brandt B,Schäfer-Korting M,Höltje HD

    更新日期:2008-02-01 00:00:00

  • Comparative investigation of the in vitro inhibitory potencies of 13-epimeric estrones and D-secoestrones towards 17β-hydroxysteroid dehydrogenase type 1.

    abstract::The inhibitory effects of 13-epimeric estrones, D-secooxime and D-secoalcohol estrone compounds on human placental 17β-hydroxysteroid dehydrogenase type 1 isozyme (17β-HSD1) were investigated. The transformation of estrone to 17β-estradiol was studied by an in vitro radiosubstrate incubation method. 13α-Estrone inhibi...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2016.1204610

    authors: Herman BE,Szabó J,Bacsa I,Wölfling J,Schneider G,Bálint M,Hetényi C,Mernyák E,Szécsi M

    更新日期:2016-01-01 00:00:00

  • In vivo experimental approach to treatment against tabun poisoning.

    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

    pub_type: 杂志文章

    doi:10.3109/14756360903357593

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

    更新日期:2010-08-01 00:00:00

  • A new class of 2-(4-cyanophenyl amino)-4-(6-bromo-4-quinolinyloxy)-6-piperazinyl (piperidinyl)-1,3,5-triazine analogues with antimicrobial/antimycobacterial activity.

    abstract::This study presents the synthesis and in vitro pharmacological evaluations of novel 2-(4-cyanophenyl amino)-4-(6-bromo-4-quinolinyloxy)-6-piperazinyl (piperidinyl)-1,3,5-triazines. The title compounds were assayed for their in vitro antimicrobial activity against eight bacteria (Staphylococcus aureus, Bacillus cereus,...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.3109/14756366.2011.592491

    authors: Patel RV,Kumari P,Rajani DP,Chikhalia KH

    更新日期:2012-06-01 00:00:00

  • Design, synthesis of 4-aminoquinoline-derived thiazolidines and their antimalarial activity and heme polymerization inhibition studies.

    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

    pub_type: 杂志文章

    doi:10.3109/14756366.2012.666537

    authors: Solomon VR,Haq W,Srivastava K,Puri SK,Katti SB

    更新日期:2013-06-01 00:00:00

  • Synthesis and cytotoxic activity against a non-small-cell bronchopulmonary carcinoma line (NSCLC-N6) of benzofuran enantiomeric derivatives.

    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

    pub_type: 杂志文章

    doi:10.1080/1475636032000069828

    authors: Hélesbeux JJ,Duval O,Séraphin D,Roussakis C,Richomme P

    更新日期:2003-04-01 00:00:00

  • QSAR study of substituted 2-pyridinyl guanidines as selective urokinase-type plasminogen activator (uPA) inhibitors.

    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

    pub_type: 杂志文章

    doi:10.1080/14756360701810355

    authors: Karthikeyan C,Moorthy NS,Trivedi P

    更新日期:2009-02-01 00:00:00

  • Structure-activity relationships of fraxamoside as an unusual xanthine oxidase inhibitor.

    abstract::Fraxamoside, a macrocyclic secoiridoid glucoside featuring a hydroxytyrosol group, was recently identified as a xanthine oxidase inhibitor (XOI) comparable in potency in vitro to the standard antigout drug allopurinol. However, this activity and its considerably higher value than its derivatives oleuropein, oleoside 1...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2016.1252758

    authors: Vitale RM,Antenucci L,Gavagnin M,Raimo G,Amodeo P

    更新日期:2017-12-01 00:00:00

  • Isoxazol-5(2H)-one: a new scaffold for potent human neutrophil elastase (HNE) inhibitors.

    abstract::Human neutrophil elastase (HNE) is an important target for the development of novel and selective inhibitors to treat inflammatory diseases, especially pulmonary pathologies. Here, we report the synthesis, structure-activity relationship analysis, and biological evaluation of a new series of HNE inhibitors with an iso...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2017.1326915

    authors: Vergelli C,Schepetkin IA,Crocetti L,Iacovone A,Giovannoni MP,Guerrini G,Khlebnikov AI,Ciattini S,Ciciani G,Quinn MT

    更新日期:2017-12-01 00:00:00

  • Monitoring the inhibitive effect of the static magnetic field on the activity of lysozyme with acoustic wave impedance analysis technique.

    abstract::The inhibitive effect of static magnetic field on the activity of lysozyme was studied using acoustic wave impedance analysis technique. Equivalent circuit parameters of piezoelectric quartz crystal (PQC) were obtained and discussed. The results showed that the activity of lysozyme was inhibited due to the effect of s...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756360410001733720

    authors: Zhang S,Wei W,Tao H,Zhang J,Mao Y

    更新日期:2004-10-01 00:00:00

  • Measurement of antioxidant ability of melatonin and serotonin by the DMPD and CUPRAC methods as trolox equivalent.

    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

    pub_type: 杂志文章

    doi:10.1080/14756360701626223

    authors: Gulçin I

    更新日期:2008-12-01 00:00:00

  • 4-Aryliden-2-methyloxazol-5(4H)-one as a new scaffold for selective reversible MAGL inhibitors.

    abstract::This study reports on a preliminary structure-activity relationship exploration of 4-aryliden-2-methyloxazol-5(4H)-one-based compounds as MAGL/FAAH inhibitors. Our results highlight that this scaffold may serve for the development of selective MAGL inhibitors. A 69-fold selectivity against MAGL over FAAH was achieved ...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.3109/14756366.2015.1010530

    authors: Granchi C,Rizzolio F,Bordoni V,Caligiuri I,Manera C,Macchia M,Minutolo F,Martinelli A,Giordano A,Tuccinardi T

    更新日期:2016-01-01 00:00:00

  • In vivo antiaging effects of alkaline water supplementation.

    abstract::Telomeres length and telomerase activity are currently considered aging molecular stigmata. Water is a major requirement for our body and water should be alkaline. Recent reports have shown that aging is related to a reduced water intake. We wanted to investigate the effect of the daily intake of alkaline water on the...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2020.1733547

    authors: Logozzi M,Mizzoni D,Di Raimo R,Andreotti M,Macchia D,Spada M,Fais S

    更新日期:2020-12-01 00:00:00

  • Biochemical characterization of the chloroplastic β-carbonic anhydrase from Flaveria bidentis (L.) "Kuntze".

    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

    pub_type: 杂志文章

    doi:10.3109/14756366.2013.813942

    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

  • In vitro inhibitory effects of some heavy metals on human erythrocyte carbonic anhydrases.

    abstract::The inhibition of two human carbonic anhydrase (HCA, EC 4.2.1.1) isozymes, the cytosolic HCA I and II, with heavy metal salts of Pb(II), Co(II) and Hg(II) has been investigated. Human erythrocyte CA-I isozyme was purified with a specific activity of 920 EUmg(-1) and a yield of 30% and CA-II isozyme was purified with a...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756360601176048

    authors: Ekinci D,Beydemir S,Küfrevioğlu OI

    更新日期:2007-12-01 00:00:00