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关键词:'oxazoles'
显示 31-60 共 1138 条结果 关于 "oxazoles" 范围 论文
Johanna Senger et al.
Journal of medicinal chemistry, 59(4), 1545-1555 (2015-12-15)
Histone deacetylase 6 (HDAC6) catalyzes the removal of an acetyl group from lysine residues of several non-histone proteins. Here we report the preparation of thiazole-, oxazole-, and oxadiazole-containing biarylhydroxamic acids by a short synthetic procedure. We identified them as selective
Thiazole and oxazole peptides: biosynthesis and molecular machinery.
R S Roy et al.
Natural product reports, 16(2), 249-263 (1999-05-20)
Arthur Y Shaw et al.
Tetrahedron letters, 53(15), 1998-2000 (2013-04-06)
This Letter discloses a novel concise synthesis of a series of 2,4,5-trisubstituted oxazoles via a tandem Ugi/Robinson-Gabriel sequence. Herein, 2,4-dimethoxybenzylamine
Kirstin Scherlach et al.
Organic & biomolecular chemistry, 10(30), 5756-5759 (2012-03-29)
Through metabolic profiling of mutants and wild type of the endofungal bacterium Burkholderia rhizoxinica two novel rhizoxin derivatives with unusual nitrile substitutions were discovered. The nitrile groups result from a photochemical oxidative cleavage of the oxazolyl moiety. In vitro studies
Xiaoyun Lu et al.
European journal of medicinal chemistry, 49, 164-171 (2012-01-24)
A series of substituted 4-(2,6-dichlorobenzyloxy)phenyl thiazole, oxazole and imidazole derivatives were synthesized. The derivatives were screened for in vitro anti-tubercular activities against Mycobacterium tuberculosis H37Rv using the Microplate Alamar Blue Assay (MABA), and antibacterial activities with agar dilution method against
Björn Kusebauch et al.
Chembiochem : a European journal of chemical biology, 12(15), 2284-2288 (2012-10-30)
Chain armor against tumor cells: The oxazole side chain in the antimitotic agent rhizoxin S2 (1) was successfully replaced through mutasynthesis by using an engineered mutant impaired in heterocyclization. Incorporation of 12 non-natural surrogates into fully processed rhizoxin analogues revealed
Monica de Gaetano et al.
European journal of medicinal chemistry, 162, 80-108 (2018-11-13)
Lipoxins (LXs) are endogenously generated eicosanoids with potent bio-actions consistent with attenuation of inflammation. The costly synthesis and metabolic instability of LXs may limit their therapeutic potential. Here we report the synthesis and characterization of novel imidazole-/oxazole-containing synthetic-LX-mimetics (sLXms). The
Garrett C Moraski et al.
European journal of medicinal chemistry, 45(5), 1703-1716 (2010-02-02)
During the syntheses and studies of natural iron chelators (mycobactins), we serendipitously discovered that a simple, small molecule, oxazoline-containing intermediate 3 displayed surprising anti-tuberculosis activity (MIC of 7.7 microM, average). Herein we report elaboration of SAR around this hit as
Atul Kumar et al.
European journal of medicinal chemistry, 44(1), 109-116 (2008-04-26)
A series of 2-aryl-naphtho[1,2-d]oxazole derivatives have been synthesized and evaluated for PTP-1B inhibitory activity. The compounds have been screened in vivo for antidiabetic activity under sucrose loaded model (SLM), sucrose-challenged streptozotocin-induced diabetic rat model (STZ-S) and db/db mice model. Compounds
Xin-Hua Liu et al.
European journal of medicinal chemistry, 44(10), 3930-3935 (2009-05-09)
Microwave irradiation promotes the rapid O,N-acylation-cyclodehydration cascade reaction of oximes and acid chloride. Twenty novel 2,4,5-trisubstituted oxazole derivatives containing heterocycle moiety were synthesized and evaluated for their antiproliferative activity. The twenty compounds are all first reported and their structures were
Anxiolytic sedatives. 1. Synthesis and pharmacology of benzo[6,7]-1,4-diazepino[5,4-b]oxazole derivatives and analogs.
T Miyadera et al.
Journal of medicinal chemistry, 14(6), 520-526 (1971-06-01)
J Espada et al.
The Histochemical journal, 27(4), 318-322 (1995-04-01)
The N-quaternized derivative of dimethyl-POPOP (termed Q4) induces a bluish-green fluorescent reaction in mast cell granules from paraffin sections and cell smears, in addition to a previously described bluish-white fluorescent reaction in chromatin DNA. The chromatin reaction was abolished by
Dawid Siodłak et al.
The journal of physical chemistry. B, 118(9), 2340-2350 (2014-02-18)
Oxazole ring occurs in numerous natural peptides, but conformational properties of the amino acid residue containing the oxazole ring in place of the C-terminal amide bond are poorly recognized. A series of model compounds constituted by the oxazole-amino acids occurring
Kelly E Desino et al.
Journal of medicinal chemistry, 52(23), 7537-7543 (2009-09-05)
Compounds that interact with microtubules, such as paclitaxel, have been shown to possess protective properties against beta-amyloid (Abeta) induced neurodegeneration associated with Alzheimer's disease. In this work, the novel agent (3R,5S,7as)-(3,5-bis(4-fluorophenyl)tetrahydro-1H-oxazolo[3,4-c]oxazol-7a-yl)methanol was investigated for effectiveness in protecting neurons against several
Yusuke Oka et al.
Bioorganic & medicinal chemistry letters, 22(24), 7534-7538 (2012-11-06)
A novel series of 2-aminothiazole-oxazoles was designed and synthesized as part of efforts to develop potent phosphoinositide 3-kinase γ (PI3Kγ) inhibitors. The modification of a high-throughput screening hit, compound 1, resulted in the identification of compounds 10 and 15, which
Matthew W Powner et al.
Journal of the American Chemical Society, 134(33), 13889-13895 (2012-07-31)
We propose a novel pathway for the prebiotic synthesis of 2'-deoxynucleotides. Consideration of the constitutional chemical relationships between glycolaldehyde and β-mercapto-acetaldehyde, and the corresponding proteinogenic amino acids, serine and cysteine, led us to explore the consequences of the corresponding sulfur
Fatma Cevik et al.
Bulletin of environmental contamination and toxicology, 80(3), 247-250 (2008-01-15)
Fenoxaprop-p-ethyl, a herbicide that is commonly used in Cukurova region, was studied for possible adverse impacts on the Seyhan dam plankton and water quality variables in laboratory microcosms for 40 days. Water containing natural plankton, and sediment were collected from
Amol V Gadakh et al.
Bioorganic & medicinal chemistry letters, 20(18), 5572-5576 (2010-08-21)
A series of fluorine containing 4-(substituted-2-hydroxybenzoyl) pyrazoles and pyrazolyl benzo[d]oxazoles were synthesized and evaluated for their antibacterial activity against Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and Bacillus subtilis and antifungal activity against Candida albicans. The antibacterial activities were expressed as
Amino group protection in peptide synthesis. The 4,5-diphenyl-4-oxazolin-2-one group.
J C Sheehan et al.
The Journal of organic chemistry, 38(17), 3034-3040 (1973-08-24)
[A method for the recovery of dioxane, naphthalene, PPO and POPOP from used scintillation solutions].
G Merkel et al.
Zeitschrift fur medizinische Laboratoriumsdiagnostik, 28(5), 279-279 (1987-01-01)
N A Meanwell et al.
Journal of medicinal chemistry, 36(24), 3871-3883 (1993-11-26)
The 4,5-diphenyloxazole derivatives 2-4 were previously identified as nonprostanoid prostacyclin (PGI2) mimetics. A series of derivatives of 2-4 bearing substitutents at the carbon atom alpha to the oxazole ring were synthesized and evaluated as inhibitors of ADP-induced aggregation of human
Wei Huang et al.
Chembiochem : a European journal of chemical biology, 12(6), 932-941 (2011-03-05)
Structurally well defined, homogeneous glycopeptides and glycoproteins are indispensable tools for functional glycomics studies. By screening of various endo-β-N-acetylglucosaminidases through the use of appropriate synthetic donor and acceptor substrates, we have found that the Flavobacterium meningosepticum endo-β-N-acetyl-glucosaminidases (GH family 18)
Montasser Hijazi et al.
Biotechnology and bioengineering, 116(2), 272-282 (2018-11-27)
A great limitation for the usability of free enzymes in organic solvents is their insolubility in these media. Some surfactants are capable of solubilizing enzymes in such media, but they are hard to remove. Covalent modification of enzymes with polymers
T Konosu et al.
Chemical & pharmaceutical bulletin, 38(9), 2476-2486 (1990-09-01)
Triazole compounds with an oxazolidine ring were designed and synthesized as a potential inhibitor of the fungal cytochrome P450 14 alpha-demethylase. In testing for antifungal activity against a mouse systemic Candida albicans infection, (4R,5R)-3-acyl-4-methyloxazolidine derivatives 4 exhibited remarkably high efficacy
Froylán Ibarra-Velarde et al.
Annals of the New York Academy of Sciences, 1149, 183-185 (2009-01-06)
The aim of the present study was to evaluate the fasciolicide activity of three experimental drugs, selected by an in silico system called TOMOCOMD-CARDD, in sheep. Drugs were identified by the computer system, and, after statistical selection, 24 Pelibuey sheep
Design and synthesis of modular oxazoline ligands for the enantioselective chromium-catalyzed addition of allyl bromide to ketones.
Jeremie J Miller et al.
Journal of the American Chemical Society, 129(10), 2752-2753 (2007-02-21)
Ralf Nauen et al.
Pest management science, 62(5), 379-382 (2006-03-24)
The mode of action of the 2,4-diphenyl-1,3-oxazoline acaricide/insecticide etoxazole has been argued to be moulting inhibition, but experimental results supporting this hypothesis are lacking. This study investigated the effect of etoxazole on chitin biosynthesis in the fall armyworm, Spodoptera frugiperda
E V Burlakova et al.
Radiatsionnaia biologiia, radioecologiia, 51(6), 660-669 (2012-03-06)
A new class of substances exhibiting radioprotective and radiosensitizing effects depending on the concentration of the substance has been found. The radioprotective effect is probably due to the resonant absorption of radiation energy and its transformation into low-energy forms, as
Kelly C G Moura et al.
Bioorganic & medicinal chemistry, 20(21), 6482-6488 (2012-09-25)
Twenty-three naphthoimidazoles and six naphthoxazoles were synthesised and evaluated against susceptible and rifampicin- and isoniazid-resistant strains of Mycobacterium tuberculosis. Among all the compounds evaluated, fourteen presented MIC values in the range of 0.78 to 6.25 μg/mL against susceptible and resistant
Montasser Hijazi et al.
Chembiochem : a European journal of chemical biology, 21(6), 874-882 (2019-10-16)
Poly(2-oxazoline)s (POxs) with 2,2'-iminodiacetate (IDA) end groups were investigated as inhibitors for laccase. The polymers with the IDA end groups are reversible, competitive inhibitors for this enzyme. The IC50 values were found to be in a range of 1-3 mm. Compared
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