Treatment of 3-aminopyridine adenine dinucleotide phosphate with sodium periodate in the neutral pH resulted in oxidation of the ribose linked to 3-aminopyridine and cleavage of the dinucleotide into adenosine and 3-aminopyridine-containing moieties. Separation of these moieties was afforded by ...

Based on the roles of Raf1 and JNK1 in hepatocarcinoma development, scaffold-based drug design was employed to produce a series of compounds, which subsequently were synthesized and explored as potential dual inhibitors Raf1 and JNK1 kinases for anti-tumor treatment. The compound 1-(3-chloro-4-(...

In the present investigation synthesis of some novel 1-(2-(1H-benzimidazol-2-yl)phenyl)-3-chloro-4-(Un/substitutedphenyl)azetidin-2-one (3a–3h) is reported. All these compounds were characterized by IR, Mass, 1H NMR and elemental analysis. The newly synthesized compounds were screened for analg...

Catalytic reactions of zeolites occur mainly at their acid sites; however, there is a lack of comprehensive method to characterize the acid sites by multiple aspects due to their complexity associated with both the host structures and the origins of formation. Here we propose a comprehensive com...

Muscles from the chick, composed primarily of αR, βR, or αW fibers, were compared with regard to whole muscle succinic dehydrogenase (SDH) activity, mitochondrial protein yield, mitochondrial SDH activity, and the ability of isolated mitochondria to oxidize α-glycerol phosphate and β-hydrox...

In a recent report, we demonstrated that intracerebral injections of the pleiotropic cytokine, ciliary neurotrophic factor (CNTF), into developing postnatal rats evoked a severe inflammatory response as determined by the appearance of reactive astrocytes and activated microglia. Considering the ...

The purpose of this study was to re-assess the classification in vivo of a series of (-)-normetazocine derivatives as κ-opioid agonists. From their ability to inhibit contractions of the electrically stimulated rabbit vas deferens, the (2″S)-N-(2″-methoxypropyl) and N-(2″-methoxyisobutyl) de...

As a part of a study to exploit anthracycline glycosides effective against resistant tumor cells, the 3′-O-methyl (3), 4′-O-methyl (4), 3′-deoxy (6), 3′-deoxy-3′-fluoro (7), and 3′-deoxy-3′-iodo (8) derivatives of 7-O-(2,6-dideoxy-2-fluoro-α-l-talopyranosyl)daunomycinone have been prepar...

The solution conformation of 4-demethoxy-7-O-[2,6-dideoxy-4-O-(2,3,6-trideoxy-3-amino-α-l-lyxo-hexopyranosyl)-α-l-lyxo- hexopyranosyl]adriamicinone, the first doxorubicin disaccharide analogue to be reported, has been analysed using nuclear magnetic resonance data and molecular mechanics calcu...

An improved synthetic approach to 7-[3-amino-4-O-(α-l-mycarosyl)-2,3,6-trideoxy-α-l-lyxo-hexopyranosyl]daunorubicinone (α1) with high stereoselectivity and good yield was developed. The feature of its binding to human serum albumin (HSA) was also investigated under simulative physiological co...

An enantioselective aldol reaction of aryl methyl ketones with aryl trifluoromethyl ketones catalyzed by tertiary amino thiourea has been established. Under mild conditions, the corresponding β-trifluoromethyl-β-hydroxy ketone products were obtained with up to 89% ee.

2-(Trifluoromethyl)furanones were obtained in good yields via the Claisen condensation of acetophenones with methyl 2-methoxytetrafluoropropionate, followed by sulfuric acid-mediated deprotection of the reaction products. These compounds react with 2,3-diaminopyridine, o-phenylenediamine and 2,3...

Unlike the hydrocarbon analogs, this first report of enolboration–aldolization of 3,3,3-trifluoropropanoic acid provides essentially pure anti-diastereomers of α-trifluoromethyl-β-hydroxy carboxylic acids in 77–90% yields.

2-(Trifluoroacetyl)chromones and 5-aryl-2-hydroxy-2-(trifluoromethyl)furan-3(2H)-ones were obtained in good yields via the Claisen condensation of acetophenones with methyl 2-methoxytetrafluoropropionate, followed by sulfuric acid-mediated deprotection of the reaction products.

Starting from 1,3-dinitro-5-trifluoromethylbenzene, a pioneering synthesis and dimethylaminomethylation of new 2-aryl-4-hydroxy-6-trifluoromethylindoles have been performed. The study of fungicidal activity has revealed the effect of dimethylaminomethyl group position on fungitoxic properties.

2-(Trifluoromethyl)butan-4-olides 13 and 14 were prepared by a three-step synthesis starting from a Wittig reagent and methyl 3,3,3-trifluoropyruvate (1) as a building block. The Wittig reaction of (2-oxoalkyl)triphenylphosphonium bromides with pyruvate 1 gave intermediate 4-oxobutenoates 8 and ...

The 1H NMR spectrum obtained with the α- and β-anomers of d-[1-2H]fructose 6-phosphate generated from d-glucose 6-phosphate sequentially exposed in D2O to phosphoglucoisomerase, phosphoglucoisomerase, phosphofructokinase and fructose-1,6-diphosphatase differed from that recorded when the deute...

The dichloro-analogue of D-fructose 1,6-bisphosphate, 1,6-dichloro-1,6-dideoxy-D-fructose, is a weak substrate for boar sperm aldolase which converts it to (S)-3-chlorolactaldehyde and 3-chloro-l-hydroxypropanone in vitro. Production of these chloro-trioses leads to the strong inhibition of glyc...

Kinetic parameters for entry of d-fructose into Trypanosoma brucei brucei have been determined. The net uptake of d-fructose was found to be rapid and occurred at a rate which was comparable with that observed for uptake of d-glucose. The Km and max were 3.91 ± 1.58 mM and 69.1 ± 7.2 nmol min−...

Allitol was produced from d-fructose via a new NADH-regenerating enzymatic reaction system using d-tagatose 3-epimerase (d-TE), ribitol dehydrogenase (RDH), and formate dehydrogenase (FDH). d-Fructose was epimerized to d-psicose by the d-TE of Pseudomonas cichorii ST-24 and the d-psicose was sub...