Antioxidant phenylpropanoid glycosides from Buddleja davidii.

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：:The activation of the β-class carbonic anhydrases (CAs, EC 4.2.1.1) from the bacteria Brucella suis and Francisella tularensis with amine and amino acids was investigated. BsuCA 1 was sensitive to activation with amino acids and amines, whereas FtuCA was not. The most effective BsuCA 1 activators were L-adrenaline and...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Angeli A,Del Prete S,Pinteala M,Maier SS,Donald WA,Simionescu BC,Capasso C,Supuran CT

更新日期：2019-12-01 00:00:00

abstract：:In the presence of the anionic surfactant sodium n-dodecyl sulphate (SDS), horseradish peroxidase (HRP) undergoes a deactivation process. Suicide inactivation of horseradish peroxidase by hydrogen peroxide(3 mM) was monitored by the absorbance change in product formation in the catalytic reaction cycle. The progress c...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Nazari K,Mahmoudi A,Shahrooz M,Khodafarin R,Moosavi-Movahedi AA

更新日期：2005-06-01 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 discovery of antibiotics as specific and effective drugs against infectious agents has generated the belief that the famous Paul Erlich theory on magic bullet should be applied to cancer as well. However, after around 60 years of failures in finding a magic bullet against cancer, a question appears mandatory: does...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Fais S

更新日期：2016-12-01 00:00:00

abstract：:A novel series of 5-(5-nitrofuran-2-yl)-and 5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazole-2-amines bearing acyclic amine at C-2 position of thiadiazole ring were synthesized and evaluated in vitro against promastigote and amastigote forms of Leishmania major. The structure-activity of series was investigated by studying ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Tahghighi A,Emami S,Razmi S,Rezazade Marznaki F,Kabudanian Ardestani S,Dastmalchi S,Kobarfard F,Shafiee A,Foroumadi A

更新日期：2013-08-01 00:00:00

abstract：:The tumor-associated transmembrane carbonic anhydrase (CA, EC 4.2.1.1) isozymes IX (CA IX) and XII (CA XII) are involved in acidification of hypoxic tumors, a process correlated with poor prognosis and clinical outcome of patients harboring such tumors. This process may be reversed by inhibiting these enzymes with pot...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Pastorekova S,Vullo D,Casini A,Scozzafava A,Pastorek J,Nishimori I,Supuran CT

更新日期：2005-06-01 00:00:00

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

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

更新日期：2008-08-01 00:00:00

abstract：:The increasing prevalence of drug resistant bacteria is a pandemic problem. Metallo-β-lactamases (MBLs) are one of the main causes of drug resistance due to hydrolysis of β-lactam antibiotics. Thus, the development of effective inhibitors of MBLs remains urgent. The compound thiomaltol was used as a lead compound to i...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Schlesinger SR,Bruner B,Farmer PJ,Kim SK

更新日期：2013-02-01 00:00:00

abstract：:The antioxidant activity of extracts from Caesalpinia sappan L. (CSL) was studied in vitro by evaluating the total phenolics, measuring the antioxidant activity by TEAC, measuring the scavenging effects on reactive oxygen species (ROS) and on reactive nitrogen species (RNS), and measuring the inhibitory effect on Cu(2...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Lee MJ,Lee HS,Kim H,Yi HS,Park SD,Moon HI,Park WH

更新日期：2010-10-01 00:00:00

abstract：:Corticosteroids are anti-inflammatory drugs that are similar to the natural corticosteroid hormones produced by the cortex of the adrenal glands. The objective of this study was to scrutinize effects of some corticosteroids on glucose-6-phosphate dehydrogenase (G6PD) and some antioxidant enzymes. Initially, G6PD was p...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ozmen I

更新日期：2005-02-01 00:00:00

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

authors： Ekinci D,Beydemir S,Küfrevioğlu OI

更新日期：2007-12-01 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：: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

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

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

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

abstract：:Initial velocity enzyme kinetics was used to study the inhibition mechanism of guanidine hydrochloride (Gdm.Cl) on catalytic activity of recombinant human protein disulfide isomerase (rhPDI) in protein folding. Reduced C125A recombinant human interleukin 2 (C125A rhIL-2), the substrate, was dissolved in 8 M Gdm.Cl bef...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Du C,Wolfe JL

更新日期：2003-02-01 00:00:00

abstract：:From the aerial parts of Thymus sibthorpii Bentham (Lamiaceae), five flavonoids apigenin (1), 7-methoxy-apigenin (2), naringenin (3), eriodictyol (4) and eriodictyol-7-glucoside (5), have been isolated together with caffeic acid methyl ester (6), rosmarinic acid (7) and rosmarinic acid methyl ester (8). The structures...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kontogiorgis C,Ntella M,Mpompou L,Karallaki F,Athanasios P,Hadjipavlou-Litina D,Lazari D

更新日期：2016-01-01 00:00:00

abstract：:This study investigates the effect of three new platinum complexes: Pt2(2,4-dimethylpyridine)4(berenil)2 (Pt14), Pt2(3,4-dimethylpyridine)4(berenil)2 (Pt15) and Pt2(3,5-dimethylpyridine)4(berenil)2 (Pt16) on growth and viability of breast cancer cells and their putative mechanism(s) of cytotoxicity. Cytotoxicity was m...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Czarnomysy R,Bielawski K,Muszynska A,Bielawska A,Gornowicz A

更新日期：2016-01-01 00:00:00

abstract：:A series of new 2,4-bis[(substituted-aminomethyl)phenyl]quinoline, 1,3-bis[(substituted-aminomethyl)phenyl]isoquinoline, and 2,4-bis[(substituted-aminomethyl)phenyl]quinazoline derivatives was designed, synthesised, and evaluated in vitro against three protozoan parasites (Plasmodium falciparum, Leishmania donovani, a...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Guillon J,Cohen A,Boudot C,Valle A,Milano V,Das RN,Guédin A,Moreau S,Ronga L,Savrimoutou S,Demourgues M,Reviriego E,Rubio S,Ferriez S,Agnamey P,Pauc C,Moukha S,Dozolme P,Nascimento SD,Laumaillé P,Bouchut A,Azas

更新日期：2020-12-01 00:00:00

abstract：:An efficient and simple microwave assisted synthesis of sulfonamide derivatives incorporating the pyridazine moiety has been developed. These sulfonamides were used for the preparation of new heterocyclic compounds via reaction with different reagents using a microwave irradiation technique. The structures of the newl...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Mohamed MI,Zaky HT,Kandile NG

更新日期：2013-12-01 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：:New anticancer agents are highly needed to overcome cancer cell resistance. A novel series of pyrimidine pyrazoline-anthracene derivatives (PPADs) (4a-t) were designed and synthesised. The anti-liver cancer activity of all compounds was screened in vitro against two hepatocellular carcinoma (HCC) cell lines (HepG2 and...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ahmed NM,Youns M,Soltan MK,Said AM

更新日期：2019-12-01 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：:The CHCl(3)-soluble fraction of the whole plant of Duranta repens showed anti-plasmodial activity against the chloroquine-sensitive (D6) and chloroquine-resistant (W2) strains of Plasmodium falciparum, with IC(50) values of 8.5 ± 0.9 and 10.2 ± 1.5 μg/mL, respectively. From this fraction, two new flavonoid glycosides,...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ijaz F,Ahmad N,Ahmad I,ul Haq A,Wang F

更新日期：2010-12-01 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：: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

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：:Adult male ICR mice were treated by intraperitoneal injection with 250 mg/kg of bodyweight of commercial malathion (a dose corresponding to 1/12 the LD50). After 6 h, acetylcholinesterase (AChE) activity in blood, liver, and six brain regions was determined. A statistically significant inhibition was observed in whole...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Banasik M,Stedeford T,Persad AS,Ueda K,Tanaka S,Muro-Cacho C,Harbison RD

更新日期：2003-12-01 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：:A trypsin inhibitor isolated from tamarind seed (TTI) has satietogenic effects in animals, increasing the cholecystokinin (CCK) in eutrophy and reducing leptin in obesity. We purified TTI (pTTI), characterised, and observed its effect upon CCK and leptin in obese Wistar rats. By HPLC, and after amplification of resolu...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Medeiros AF,Costa IS,Carvalho FMC,Kiyota S,Souza BBP,Sifuentes DN,Serquiz RP,Maciel BLL,Uchôa AF,Santos EAD,Morais AHA

更新日期：2018-12-01 00:00:00