We examine (z, Z)-type contracts for vendor-managed inventory (VMI) between a supplier and a retailer from the retailer's perspective. A (z, Z) VMI contract specifies minimum and maximum inventory levels and their corresponding under- and over-stocking penalties. The retailer chooses the co...
Synthesis of some 5-halo-[E]-6(2-p-toluoylvinyl)uracils and some 5-alkynyl-[E]-6-(2-p-toluoylvinyl)uracils through palladium-catalysed procedure and cytotoxicities of the former and [E]-6-(2-p-toluoylvinyl)uracils are reported.
The synthesis and structure–activity relationships of a novel aryl uracil series which contains a fused 5,6-bicyclic ring unit for HCV NS5B inhibition is described. Several analogs display replicon cell culture potencies in the low nanomolar range along with excellent rat pharmacokinetic values.
A simple and novel cyclo-condensation reaction of 6-amino-uracils and isatins for the synthesis of spiro[pyrimido[4,5-b]quinoline-5,5′-pyrrolo[2,3-d]pyrimidine] derivatives is reported.
The catalytic trifluoromethylation of uracil using CF3I was investigated to find a new industrial process for the production of 5-trifluoromethyluracil. The catalytic system of FeSO4, H2O2 and H2SO4 in dimethylsulfoxide efficiently and selectively yielded 5-trifluoromethyluracil under mild condi...
P2Y receptors (P2YRs) are a family of G protein-coupled receptors activated by extracellular nucleotides. Physiological P2YR agonists include purine and pyrimidine nucleoside di- and triphosphates, such as ATP, ADP, UTP, UDP, nucleotide sugars, and dinucleotides. Eight subtypes exist, P2Y1, P2Y2...
This review article is an effort to summarize recent developments in researches providing uracil derivatives with promising biological potential. This article also aims to discuss potential future directions on the development of more potent and specific uracil analogues for various biological t...
3-Nitropyridine was reacted with ammonia or alkylamines and KMnO4 under several different conditions. Substitutions in the para position to the nitro group were obtained with high regioselectivity: with ammonia, 2-amino-5-nitropyridine (66%), with butylamine, 2-butylamino-5-nitropyridine (92%), ...
An efficient approach for the formation of 5-amino- and 7-amino-6-azaoxindole derivatives was developed. 2-Amino-4-chloro-3-nitropyridine (8), and its 5-nitro-substituted regioisomer (9), respectively, were obtained by reaction with ethyl malonate. The resulting 2-amino-3/5-nitropyridine derivat...
2-Chloropurine is attacked by mammalian xanthine oxidase simultaneously at C-6 and C-8. The ratio of the two rates (=1) is insensitive to variations of pH or temperature. Experiments with 2-chloropurine as inhibitor indicate instantaneous association of this purine with the active center of the ...
2-Chloropurine is the first purine, for which simultaneous enzymic oxidation along two different pathways has been established. Attack at either carbon atom 6 or 8 proceeds at the same rate. This phenomenon is ascribed to the mesomeric (+M) effect of the halogen in position 2, which exhibits pro...
(−)-β-d-2-Aminopurine dioxolane (APD), (−)-β-d-2-amino-6-chloropurine dioxolane (ACPD) and dioxolane guanine (DXG) are nucleoside analogues possessing potent activity against human immunodeficiency virus (HIV) and hepatitis B virus (HBV) in vitro. APD and ACPD are metabolized in vivo to yield ...
Two purine tautomers of 2-amino-6-chloropurine (ACP), in labeled as N9H10 and N7H10, were investigated by vibrational spectroscopy and quantum chemical method. The FT-IR and FT-Raman spectra of ACP have been recorded in the regions 4000–400 cm−1 and 3500–100 cm−1, respectively. The measured sp...
A novel approach to the synthesis of 6-(2-hydroxyethyl)purines was developed based on Pd-catalyzed cross-coupling reactions of 6-chloropurines with the Reformatsky reagent followed by reduction by NaBH4 and treatment with MnO2. This methodology was successfully applied to the syntheses of 6-(eth...
9-Substituted 2-amino-6-chloropurines are important intermediates in the synthesis of a variety of purine and purine nucleoside derivatives, and were efficiently halogenated, alkylated and formylated at the C-8 position via lithiation of N2 mono THP protected purines. Notably, even fluoride coul...
From a collection containing more than 1500 academic compounds, in silico screening identified a hit for the human A1 adenosine receptor containing a new purine scaffold. To study the structure activity relationships of this new chemical series for adenosine receptors, a library of 24 purines wa...
A novel set of 1,4-diaryl-1,2,3-triazoles were projected as a tool to study the effect of both the heteroaromatic triazole as a core ring and a variety of chemical groups with different electronic features, size and shape on the catalytic activity of the two COX isoenzymes. The new triazoles wer...
The paper reports the study of thermal stability and decomposition mechanisms of the newly synthesized phenyl series energetic molecule named 1-(2-methoxy,-3,5-dinitrophenyl)-1H-1,2,3-triazole (S5) using time resolved pulsed photoacoustic (PA) pyro analysis technique. The thermal PA spectra of t...
The development of copper catalyzed azide–alkyne cycloaddition in aqueous solvent system at room temperature is a notable contribution to the field of green chemistry. In this work, 1,4-disubstitued-1H-1,2,3-triazoles are synthesized in the Fehling solution, a widely used system in practical la...
Vascular endothelial growth factor (VEGF) and its receptor (VEGFR) is essential for physiological functions of tissues and neovasculature. VEGFR signaling is associated with the progression of pathological angiogenesis in various types of malignancies, making it an attractive therapeutic target ...
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