CN
Search Within
H23805
应用筛选条件
关键词:'H23805'
显示 1-30 共 36 条结果 关于 "H23805" 范围 论文
Zhou-peng Li et al.
The Journal of pharmacy and pharmacology, 67(4), 573-582 (2015-01-06)
Due to the increasing prevalence of drug-resistant Staphylococcus aureus infection, we develop novel 4-hydroxycoumarin derivatives as antimicrobials. The antibacterial activity of 4-hydroxycoumarin derivatives against drug-susceptive S. aureus (ATCC 29213) and methicillin-resistant S. aureus (MRSA) were evaluated using minimal inhibitory concentration (MIC) assay;
Leticia Mayor-López et al.
Translational oncology, 7(5), 590-604 (2014-11-13)
The use of heat shock protein 90 (Hsp90) inhibitors is an attractive antineoplastic therapy. We wanted to compare the effects of the benzoquinone 17-allylamino-17-demethoxygeldanamycin (17-AAG, tanespimycin) and the novel isoxazole resorcinol-based Hsp90 inhibitor NVP-AUY922 in a panel of pancreatic and
Stancho Stanchev et al.
European journal of medicinal chemistry, 43(4), 694-706 (2007-07-07)
Six new 4-hydroxycoumarin derivatives have been synthesized. They were characterized by UV-vis, IR, (1)H NMR, (13)C NMR, mass spectral data, elemental analysis, TLC and melting point determination. The new 4-hydroxycoumarin derivatives are studied by computational methods--DFT (B3LYP) and force field
Karen A Nolan et al.
Journal of medicinal chemistry, 52(22), 7142-7156 (2009-11-03)
The synthesis is reported here of two novel series of inhibitors of human NAD(P)H quinone oxidoreductase-1 (NQO1), an enzyme overexpressed in several types of tumor cell. The first series comprises substituted symmetric dicoumarol analogues; the second series contains hybrid compounds
Anna Maria Ferrari et al.
European journal of medicinal chemistry, 42(7), 1028-1031 (2007-02-24)
Quantum-chemical descriptors related to proton dissociation constants of a set of coumarins hydroxylated in various positions have been computed and related to the experimental pK(a) values. An excellent correlation was found between the computed deprotonation energies of hydroxycoumarins in water
Susan Chen et al.
Journal of chromatographic science, 52(8), 950-953 (2013-08-01)
Column-related carryover affects both accuracy and precision in liquid chromatography-tandem mass spectrometry (LC-MS/MS) analysis. In this work, a novel straightforward dynamic flush method to reduce the column-related carryover was developed by alternating the column flow direction of liquid chromatographic separation
Davorka Zavrsnik et al.
Bosnian journal of basic medical sciences, 8(3), 277-281 (2008-09-26)
Due to exceptional reactivity of 4-hydroxycoumarin, the synthesis of new coumarin derivatives of dimer and tetramer type has been carried out. The synthesis was carried out from 4-hydroxycoumarin and various aromatic aldehydes. In this way, compounds of the dimer 3,3'-(benzilidene)bis
Atsushi Kato et al.
Bioorganic & medicinal chemistry letters, 20(19), 5630-5633 (2010-09-02)
We report the structure-activity relationship of a series of coumarins as aldose reductase 2 (ALR2) inhibitors and their suppressive effect on the accumulation of galactitol in the rat lens. We evaluated their ALR2 selectivity profile against sorbitol dehydrogenase and aldehyde
Ayoob Bazgir et al.
Ultrasonics sonochemistry, 17(2), 447-452 (2009-10-20)
A simple, facile, efficient and three-component procedure for the synthesis of spiro[indoline-3,4'-pyrazolo[3,4-b]pyridine]-2,6'(1'H)-diones by the reaction of 4-hydroxycumarin, isatins and 1H-pyrazol-5-amines in water under ultrasonic irradiation is reported. The advantages of this method are the use of an inexpensive and readily
Pei-Yu Kuo et al.
Molecular diversity, 13(2), 253-260 (2009-02-03)
3-Benzoyl-7-dimethylamino-4-hydroxycoumarin was synthesized and its UV-vis spectra in various mixtures of MeOH and CH(2)Cl(2) were measured. The diketone lactone exists mainly in the exocyclic-enol form in protic solvents and the endocyclic-enol form in nonpolar solvents. Acetylation, amination and methylation products
Lulzime Ballazhi et al.
Acta pharmaceutica (Zagreb, Croatia), 65(1), 53-63 (2015-03-18)
The study highlights the current progress in the development of coumarin scaffolds for drug discovery as novel anticancer agents in metastatic breast cancer. Eight compounds, combining the coumarin core and five membered heterocycles (isoxazoles and thiazoles) in hydrazinyldiene- -chroman-2,4-diones, were
Ian A Nicholls et al.
Journal of molecular recognition : JMR, 23(6), 604-608 (2010-10-30)
The complex nature of the structure of the anticoagulant warfarin is reflected in the diversity of binding modes observed in warfarin-protein recognition systems. A series of theoretical, (1)H-NMR and steady state and time resolved fluorescence spectroscopic studies, have been used
Yan Sun et al.
Molecular diversity, 16(1), 163-171 (2011-12-01)
An efficient synthetic method for the densely substituted 3-arylaminoacrylates was successfully developed via the one-pot reaction of arylamines, methyl propiolate, aromatic aldehydes, and active methylene compounds such as pivaloylacetonitrile, 1,3-cyclopentanedione, and 4-hydroxycoumarin. The key step of the reaction was believed
Vassiliki Panteleon et al.
Bioorganic & medicinal chemistry letters, 18(21), 5781-5784 (2008-10-07)
A series of novel spiro-substituted 4-hydroxypyranocoumarins and their corresponding dihydropyrano cis-diols has been synthesized. Among them the spiroadamantylpyranocoumarin and the diols can interact with the stable free radical 1,1-diphenyl-2-picrylhydrazyl and scavenge superoxide anions generated in the xanthine-xanthine oxidase system.
Davood Nematollahi et al.
Chemical & pharmaceutical bulletin, 56(11), 1562-1566 (2008-11-05)
The 4-(dihydroxyphenylthio)-2H-chromen-2-one derivatives have been synthesized by direct electrochemical oxidation of catechols in the presence of 4-mercaptocoumarin as a nucleophile in water/acetonitrile (50/50) solution, in a one-pot process, at carbon rod electrode, in an undivided cell and in constant current
Changning Wang et al.
Journal of medicinal chemistry, 54(7), 2331-2340 (2011-03-12)
Myelination represents one of the most fundamental biological processes in the vertebrate nervous system. Abnormalities and changes in myelination in the central nervous system (CNS) are seen in many neurodegenerative disorders, such as multiple sclerosis (MS). A long-standing goal has
Alfonso Maresca et al.
Bioorganic & medicinal chemistry letters, 20(15), 4511-4514 (2010-06-29)
A series of coumarins incorporating hydroxy-, chloro- and/or chloromethyl-moieties in positions 3-, 4-, 6- and 7- of the heterocyclic ring were investigated for the inhibition of the zinc enzyme carbonic anhydrase (CA, EC 4.2.1.1). These coumarins were very weak or
S Stanchev et al.
European journal of medicinal chemistry, 44(7), 3077-3082 (2008-08-30)
The aim of this investigation was to measure the activity of four 4-hydroxycoumarin derivatives - three of them were described before and one was newly synthesized. The substances were ethyl 2-[(4-hydroxy-2-oxo-2H-chromen-3-yl)(4-hydroxyphenyl)methyl]-3-oxobutanoate (SS-14), 4-[1-(4-hydroxy-2-oxo-2H-chromen-3-yl)-2-(ethoxycarbonyl)-3-oxobutyl]benzoic acid (SS-17), ethyl 2-[(4-hydroxy-2-oxo-2H-chromen-3-yl)(3-nitrophenyl)methyl]-3-oxobutanoate (SS-21) and ethyl
Katrin J Czogalla et al.
Blood, 122(15), 2743-2750 (2013-08-29)
Since the discovery of warfarin-sensitive vitamin K 2,3-epoxide reductase complex subunit 1 (VKORC1), 26 human VKORC1 (hVKORC1) missense mutations have been associated with oral anticoagulant resistance (OACR). Assessment of warfarin resistance using the "classical" dithiothreitol-driven vitamin K 2,3-epoxide reductase (VKOR)
Sergio A Rodríguez et al.
Bioorganic & medicinal chemistry, 19(21), 6233-6238 (2011-10-04)
The antioxidant activity of 4-hydroxycoumarin synthetic derivatives and 4-methylumbelliferone were determined taking 4-hydroxycoumarin as the reference compound. Six 3-aryl-4-hydroxycoumarin derivatives were synthesized from 4-hydroxycoumarin as precursor in order to evaluate changes in their antioxidant properties due to C3-aryl substituent nature.
Ana Carolina Luchini et al.
Biological & pharmaceutical bulletin, 31(7), 1343-1350 (2008-07-02)
Coumarins represent an important class of phenolic compounds with multiple biological activities, including inhibition of lipidic peroxidation and neutrophil-dependent anion superoxide generation, anti-inflammatory and immunosuppressor actions. All of these proprieties are essential for that a drug may be used in
Mikael I Naumov et al.
The Journal of organic chemistry, 72(9), 3293-3301 (2007-03-29)
2-(methoxymethoxymethyl)aryllead triacetates, obtained in situ from the corresponding arylboronic acids, reacted with 4-hydroxycoumarins, leading to 3-(2-methoxymethoxymethyl)aryl-4-hydroxycoumarin derivatives in good to high yields. These compounds underwent a cascade sequence of reactions, deprotection-halogenation-annulation, to afford polyoxygenated tetracyclic 6H,11H-[2]benzopyrano-[4,3-c] [1]benzopyran-11-ones in good yields.
Jia Zhang et al.
Journal of mass spectrometry : JMS, 47(8), 1059-1064 (2012-08-18)
A mass spectrometric study of protonated warfarin and its derivatives (compounds 1 to 5) has been performed. Losses of a substituted benzylideneacetone and a 4-hydroxycoumarin have been observed as a result of retro-Michael reaction. The added proton is initially localized
Manoj R Zanwar et al.
The Journal of organic chemistry, 77(15), 6495-6504 (2012-07-20)
The unusual alcohol mediated formation of 4-oxo-2-aryl-4H-chromene-3-carboxylate (flavone-3-carboxylate) derivatives from 4-hydroxycoumarins and β-nitroalkenes in an alcoholic medium is described. The transformation occurs via the in situ formation of a Michael adduct, followed by the alkoxide ion mediated rearrangement of the
Jae-Chul Jung et al.
Molecules (Basel, Switzerland), 17(2), 2091-2102 (2012-02-23)
The total synthesis and structure determination of cis- and trans-flocoumafen was described. The key synthetic steps involve Knoevenagel condensation with p-methoxybenzaldehyde, in situ decarboxylation and intramolecular ring cyclization to construct the tetralone skeleton. Stereospecific reduction of the O-alkylated ketone 13
Dharmesh H Mahajan et al.
Archiv der Pharmazie, 342(5), 281-290 (2009-05-06)
Novel 2-(coumarin-4-yloxy)-4,6-(substituted)-s-triazine derivatives i. e., diaryltriazine (DATA) are reported as novel non-nucleoside reverse transcriptase inhibitors (NNRTIs), were synthesized and their activities against human immunodeficiency virus HIV-1 (III-B), HIV-2 (ROD), and the double RT mutant HIV-1 (K103N and Y181C) were assessed.
Markus Gebauer
Bioorganic & medicinal chemistry, 15(6), 2414-2420 (2007-02-06)
4-Hydroxycoumarins such as warfarin 1 have been the mainstay of oral anticoagulation therapy for over 20 years. Yet little detail is known about the molecular interactions between 4-hydroxycoumarins with vitamin K epoxide reductase (VKER), inhibition of which produces a deficiency
Nohemí Salinas-Jazmín et al.
Cancer chemotherapy and pharmacology, 65(5), 931-940 (2009-08-20)
We have previously reported that in vitro treatment of B16-F10 melanoma cells with 4-hydroxycoumarin (4-HC) decreases their metastatic potential. However, the antimetastatic efficacy of 4-HC in vivo is unknown; therefore, we investigated the antimetastatic and antineoplastic effects of 4-HC in
Pen-Yuan Lin et al.
Molecules (Basel, Switzerland), 17(9), 10846-10863 (2012-09-12)
Coumarin derivatives are used as fluorescent dyes and medicines. They also have some notable physiological effects, including the acute hepatoxicity and carcinogenicity of certain aflatoxins, the anticoagulant action of dicoumarol, and the antibiotic activity of novobicin and coumerymycin A1. Because
Shizuka Saito et al.
Shokuhin eiseigaku zasshi. Journal of the Food Hygienic Society of Japan, 52(4), 244-250 (2011-08-30)
A sensitive and selective method for the determination of 4-hydroxycoumarin-type rodenticides (warfarin, coumatetralyl, bromadiolone, and brodifacoum) in animal products, fishery products, and honey was developed. 4-Hydroxycoumarin rodenticides were extracted with acidified acetone, and the crude extract was purified by liquid-liquid
1/2