Design, synthesis and pharmacological evaluation of 6-hydroxy-4-methylquinolin-2(1H)-one derivatives as inotropic agents.

abstract：:Glutathione transferase P1-1 is over expressed in some cancer cells and contributes to detoxification of anticancer drugs, leading to drug-resistant tumors. The inhibition of human recombinant GSTP1-1 by natural plant products was investigated using 10 compounds isolated from plants indigenous to Southern and Central ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Mukanganyama S,Bezabih M,Robert M,Ngadjui BT,Kapche GF,Ngandeu F,Abegaz B

更新日期：2011-08-01 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：:Photodynamic molecules represent an alternative approach for cancer therapy for their property (i) to be photo-reactive; (ii) to be not-toxic for target cells in absence of light; (iii) to accumulate specifically into tumour tissues; (iv) to be activable by a light beam only at the tumour site and (v) to exert cytotox...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kusuzaki K,Matsubara T,Murata H,Logozzi M,Iessi E,Di Raimo R,Carta F,Supuran CT,Fais S

更新日期：2017-12-01 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：: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：: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：: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

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

更新日期：2004-10-01 00:00:00

abstract：:Cyanidin-3-galactoside, a natural anthocyanin, was investigated for its alpha-glucosidase inhibitory activity. The IC(50) value of cyanidin-3-galactoside was 0.50 +/- 0.05 mM against intestinal sucrase. A low dose of cyanidin-3-galactoside showed a synergistic inhibition on intestinal alpha-glucosidase (maltase and su...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Adisakwattana S,Charoenlertkul P,Yibchok-Anun S

更新日期：2009-02-01 00:00:00

abstract：:Leishmaniasis is considered as one of the major neglected tropical diseases due to its magnitude and wide geographic distribution. Leishmania braziliensis, responsible for cutaneous leishmaniasis, is the most prevalent species in Brazil. Superoxide dismutase (SOD) belongs to the antioxidant pathway of the parasites an...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Brito CCB,Silva HVCD,Brondani DJ,Faria AR,Ximenes RM,Silva IMD,Albuquerque JFC,Castilho MS

更新日期：2019-12-01 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：:A new series of functionalized amino acid derivatives N-substituted 1-N-(tert-butoxycarbonyl)-2,2-dimethyl-4-phenyl-5-oxazolidine carboxamide (1-17) and 1-N-substituted-3-amino-2-hydroxy-3-phenylpropane-1-carboxamide (18-34) were synthesized and evaluated for their in vitro cytotoxicity against human cancer cell lines...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kumar V,Mudgal MM,Rani N,Jha A,Jaggi M,Singh AT,Sanna VK,Singh P,Sharma PK,Irchhaiya R,Burman AC

更新日期：2009-06-01 00:00:00

abstract：:A recombinant carbonic anhydrase (CA, EC 4.2.1.1) from the soil-dwelling bacterium Enterobacter sp. B13 was cloned and purified by Co(2+) affinity chromatography. Bioinformatic analysis showed that the new enzyme (denominated here B13-CA) belongs to the β-class CAs and to possess 95% homology with the ortholog enzyme ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Eminoğlu A,Vullo D,Aşık A,Çolak DN,Supuran CT,Çanakçı S,Osman Beldüz A

更新日期：2016-12-01 00:00:00

abstract：:The synthesis of a new series of imidazo[1,2-a]pyrazine-2-carboxylic acid arylidene-hydrazides is described. The chemical structures of the compounds were elucidated by IR, (1)H-NMR, FAB(+)-MS spectral data. Their biological activity against various bacteria, fungi species, and Mycobacterium tuberculosis was investiga...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ozdemir A,Turan-Zitouni G,Kaplancikli ZA,Tunali Y

更新日期：2009-06-01 00:00:00

abstract：:EGFR tyrosine kinase has been reported mainly in 40-80% of non-small lung cancers, in addition to colon and breast cancers. In this study, we illustrate the synthesis of a highly potent antitumor agent. The synthesized compound 4 was screened at NCI, USA, for antitumor activity against non-small lung cancer, colon can...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Gabr MT,El-Gohary NS,El-Bendary ER,El-Kerdawy MM

更新日期：2015-02-01 00:00:00

abstract：:Three series of sintenin derivatives (compounds 1-14) were designed and prepared and their antioxidative and neuroprotective effects were evaluated. The in vitro models of scavenging 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals, chelating ferrous ions, inhibiting the rat brain homogenates lipid peroxidation, and prot...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Yang LX,Zhang LJ,Huang KX,Kun Li X,Hu LH,Wang XY,Stockigt J,Zhao Y

更新日期：2009-04-01 00:00:00

abstract：:The hypoxic tumour microenvironment of solid tumours represents an important starting point for modulating progression and metastatic spread. Carbonic anhydrase IX (CAIX) is a known HIF-1α-dependent key player in maintaining cell pH conditions under hypoxia. We show that CAIX is strongly expressed in esophageal carcin...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Drenckhan A,Freytag M,Supuran CT,Sauter G,Izbicki JR,Gros SJ

更新日期：2018-12-01 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：: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：: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：:In this article the synthesis of new 1H-(2'-pyridyl)-3-methyl-5-hydroxypyrazole and 1H-(2'-pyridyl)-3-phenyl-5-hydroxypyrazole complexes with palladium(II) ions is reported. The structures of obtained compounds have been characterized by X-ray crystallography and DFT (density functional theory) calculations. The cytot...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ciolkowski M,Paneth P,Lorenz IP,Mayer P,Rozalski M,Krajewska U,Budzisz E

更新日期：2009-12-01 00:00:00

abstract：:Nineteen 5-nitrothiazolylthiosemicarbazones were synthesized from 5-nitrothiazole by three-step synthesis and evaluated for in vitro activities against seven mycobacterial species. Among them, N-(5-nitro-1, 3-thiazol-2-yl)-2-((Z)-4-[(phenylmethyl)oxy]phenylmethylidene)hydrazine-1-carbothioamide (4m) was found to be th...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Sriram D,Yogeeswari P,Senthilkumar P,Sangaraju D

更新日期：2010-02-01 00:00:00

abstract：:Continuous efforts to identify sEH inhibitors using activity-guided fractionation have revealed 12 known compounds, 2-13, from Rheum undulatum. Compounds 2-13 and 1, which was obtained from the in-house library, were tested for inhibitory activity against sEH. Compounds 1-9, 11, and 12 were shown to have inhibitory ac...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Jo AR,Kim JH,Yan XT,Yang SY,Kim YH

更新日期：2016-01-01 00:00:00

abstract：:In an in vitro screening for human carbonic anhydrase (hCA) inhibiting agents from higher plants, the petroleum ether and ethyl acetate extracts of Magydaris pastinacea seeds selectively inhibited hCA IX and hCA XII isoforms. The phytochemical investigation of the extracts led to the isolation of ten linear furocoumar...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Fois B,Distinto S,Meleddu R,Deplano S,Maccioni E,Floris C,Rosa A,Nieddu M,Caboni P,Sissi C,Angeli A,Supuran CT,Cottiglia F

更新日期：2020-12-01 00:00:00

abstract：:Poly(ADP-ribose) polymerase (PARP)-1 inhibitor has been suggested to attenuate the ischemia-reperfusion injury. We investigated the protective effect of the cardioplegia with a PARP-1 inhibitor, 4-hydoxyquinazoline (4-HQ), against myocardial ischemia-reperfusion injury. Isolated rat hearts were perfused on a Langendor...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Yamazaki K,Tanaka S,Sakata R,Miwa S,Oriyanhan W,Takaba K,Minakata K,Marui A,Ikeda T,Toyokuni S,Komeda M,Ueda K

更新日期：2013-02-01 00:00:00

abstract：:The acetylcholinesterase inhibitory and/or antitumour activities of amino-, thio- and ester-derivatives of avarol selected were evaluated for the first time at in vitro conditions. Avarol-3',4'-dithioglycol (1) and avarol-4'-(3)mercaptopropionic acid (3) were shown to be the best inhibitors of the enzyme tested (0.50 ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Tommonaro G,Pejin B,Iodice C,Tafuto A,De Rosa S

更新日期：2016-08-01 00:00:00

abstract：:Structure modification of the side chain of the lead compound benzoxanthone provided a series of benzoxanthone analogues and 12 of them were first reported. The results showed that most of these compounds had moderate cytotoxicity against tumour cells with the 50% inhibition concentration in the micromolar range. Furt...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Cheng P,Zhu L,Guo W,Liu W,Yao J,Dong G,Zhang Y,Zhuang C,Sheng C,Miao Z,Zhang W

更新日期：2012-06-01 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：:This paper reports the synthesis of O-methyl and O-ethyl NSAID hydroxamic acids, their antimicrobial activities, and their ability to inhibit urease and soybean lipoxygenase activities. Ibuprofen and fenoprofen hydroxamic acids with free hydroxy groups present the highest antimicrobial activity, while indomethacin and...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Rajić Z,Perković I,Butula I,Zorc B,Hadjipavlou-Litina D,Pontiki E,Pepeljnjak S,Kosalec I

更新日期：2009-10-01 00:00:00

abstract：:In a new group of 3-methyl-2-phenyl-1-substituted-indole derivatives (10a-f), the indomethacin analogs were prepared via the Fisher indole synthesis reaction of propiophenone with appropriately substituted phenylhydrazine hydrochloride. This is followed by the insertion of the appropriate benzyl or benzoyl fragment. A...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Abdellatif KR,Lamie PF,Omar HA

更新日期：2016-01-01 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