ContextAtrial and brain natriuretic peptides (ANP and BNP) are established diagnostic and prognostic markers in heart failure, but their utility in patients with advanced cancer is unclear.
BackgroundCurrent evidence indicates that measurement of pleural fluid N-terminal pro-brain natriuretic peptide (NT-proBNP) levels can aid in distinguishing pleural effusions of cardiac origin from those of noncardiac origin. To date, only one study, to our knowledge, has described simultaneous ...
This review includes the classification, nomenclature, methoda of characterization, reactivity, synthesis, and applications of three heterocyclic ring fused (5:5:5) compounds published during the period 1995 to 2005.
The nitrogen containing spiro-heterocycle is one of the privileged synthetic motif that constitutes various naturally occurring molecules and displays a broad range of pharmaceutical and biological activities. A new methodology was developed for the synthesis of 2,4-diazaspiro[5.5]undecane-1,3,5...
Rational drug design method has been used to generate 4-arylpiperazine carboxamides in an effort to develop safer, more potent and effective monoamine neurotransmitters reuptake inhibitors. Out of twenty-seven synthesized compounds, compound 9 displayed potent monoamine neurotransmitter reuptake...
One-pot sequential reactions using the acyl moieties installed by enzymatic dynamic kinetic resolution of alcohols have been little investigated. In this work, the acryloyl moiety installed via the lipase/oxovanadium combo-catalyzed dynamic kinetic resolution of a racemic dienol [4-(cyclohex-1-e...
The dinuclear zinc complexes as high performance catalysts were used to catalyze phospha-Michael reaction of exocyclic α,β-unsaturated benzocyclic ketones under mild conditions, and the desired products possessing 1-indanones or 1-tetralones skeleton were obtained with excellent enantioselecti...
Eight racemic 1-(furan-2-yl)ethanols were prepared from the corresponding carbonyl compounds for enantioselective acylation studies, and seven of them were used in preparative-scale kinetic resolutions with Candida antarctica lipase B (Novozym 435) and vinyl acetate in dried diisopropyl ether. M...
This chapter describes methods of synthesis, pharmacological properties and the use of derivatives of 4-substituted and 1,4-disubstituted piperidines such as 4-piperidinols and their derivatives, which include periciazine, diphenylpyraline, ebastine, bepotastine, lamifiban, eucatropine, propiver...
Protein aggregation follows some common motifs. Whether in the formation of inclusion bodies in heterologous overexpression systems or inclusions in protein conformational diseases, or aggregation during storage or transport of protein formulations, aggregates form cross beta-sheet structures an...
N-Thioacylation of neuraminic acid methyl α-glycoside (5) with O-ethyl thioformate (1), methyl dithioacetate (2), and methyl dithiopropionate (3) afforded N-thioformyl, N-thioacetyl, and N-thiopropionyl neuraminic acid derivatives 6a-c in high yield. Cleavage of the glycosides was accomplished ...
Avian Infectious bronchitis virus (IBV) is a coronavirus that infects chickens via the respiratory epithelium as primary target cells. The binding of coronaviruses to the cell surface is mediated by the viral surface protein S. Recently we demonstrated that α2,3-linked sialic acid serves as a r...
Herein we report the synthesis of N-acetyl neuraminic acid derivatives as 4-methylumbelliferyl glycosides and their use in fluorometrically quantifying human and bacterial sialidase activity and substrate specificities. We found that sialidases in the human promyelocytic leukemic cell line HL60 ...
SummaryPathogens such as non-typeable Haemophilus influenzae (NTHi) evade the immune system by presenting host-derived sialic acids. NTHi cannot synthesize sialic acids and therefore needs to utilize sialic acids originating from host tissue. Here we report sialic acid-based probes to visualize ...
Four isomeric hydroxy-skipped bishomo-inositol analogs have been synthesized from both enantiomers of 5-hydroxymethyl-2-cyclohexenone. Sharpless asymmetric dihydroxylation and substrate-directed anionic hydroxymethylation are the key reactions which have been employed successfully for the synthe...
A novel β-D-2′-deoxy-2′-α-fluoro-2′-β-C-(fluoromethyl)uridine phosphoramidate prodrug (1) has been synthesized. This compound exhibits submicromolar-level antiviral activity in vitro against HCV genotypes 1b, 1a, 2a, and S282T replicons (EC50 = 0.18–1.13 μM) with low cytotoxicity (CC50 >...
A new efficient method for the asymmetric synthesis of β-heterocycle substituted (2S,3S)-α-aminobutyric acids through the diastereoselective addition of 5-thioxo-4-allyl-1,2,4-triazoles, containing various substituents at the 3-position, to the CC double bond of (E)- and (Z)-dehydroaminobutyri...
A simple, fast, sensitive, and reliable method for the determination of 2-(3-benzoylphenyl)propionic acid in biological fluid is described. The method is based on a quantitative ether extraction of plasma samples followed by TLC separation, spot visualization and elution, and determination at 25...
SBA-15 ordered mesoporous silica functionalized with (3-aminopropyl)triethoxysilane (APTES) was used as the carrier for anti-inflammatory drug: 2-(3-benzoylphenyl)propionic acid – ketoprofen. The surface of SBA-15 containing free silanol groups was modified with 3-aminopropyltriethoxysilane via...
[N-(2-Benzoylphenyl)benzamido-κ2N,O](η1-benzyl)(trimethylphosphine)Ni(II) (3) is prepared by the reaction of potassium N-(2-benzoylphenyl)benzamide and Ni(η3-CH2C6H5)Cl(PMe3). When 3 is treated with one equivalent of B(C6F5)3, one obtains a zwitterionic complex, [PhC(O)C6H4NC(Ph)OB(C6F5...
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