Allopurinol-1-riboside, a major metabolite of allopurinol, is commonly thought to be directly synthesized by purine nucleoside phosphorylase (PNP) in vivo. As this enzyme is otherwise believed to function in vivo primarily in the direction of nucleoside breakdown, we have determined by high perf...

The synthesis of a mannosylated carrier used as a drug delivery system to target specifically an antileishmanial drug allopurinol riboside [4-hydroxy-1-β-D-ribofuranosyl-1H-pyrazolo(3,4-d) pyrimidine] into Leishmania donovani infected macrophages via their membrane lectin is described. The synt...

Ethylene–propylene–diene monomer (EPDM) containing 5-ethylidene-2-norbornene (ENB) as diene was exposed to an artificial weathering environment produced by a xenon lamp light exposure and weathering equipment for different time periods. The surface chemical changes were detected by Specular Re...

Several predictive models were used to assess aquatic exposure, persistence (P) and potential for long-range transport (LRT) of 5-ethylidene-2-norbornene (ENB). Such estimations are components of the assessment process for persistent, bioaccumulative and toxic (PBT) substances, which are also re...

[2, 8-13C2] ENB was synthesized from labelled acetic acid and terpolymerized in a batch reactor to [2, 8-13C2] ENB–EPDM rubber (Mw=4.8×105, d=3, ENB content ∼8 wt.%, ethene to propene ratio ∼1.8). Labelled ENB, its precursors and the EPDM were characterized by NMR spectroscopy. ENB is incorp...

Functionalized multiwalled carbon nanotubes (MWCNTs) reinforced poly(5-ethylidene-2-norbornene (ENB)) composites have been fabricated via ring-opening metathesis polymerization. Verification of covalent bond formation between the functionalized carbon nanotubes and the polyENB matrix was demonst...

Saturated olefinic rubbers have been widely used as materials for not only municipal waterworks, but also for household uses. As a sanitizing agent for water, chlorine will be replaced by ozone in the near future from an environmental point of view. However, the ozone treatment in water seriousl...

5-Ethylidene-2-norbornene (ENB) polymerization and copolymerization with ethylene (E) catalyzed by constrained geometry catalyst 2-tetramethylcyclopentadienyl-4,6-di-tert-butylphenoxytitanium dichloride (1) were studied in the presence of AliBu3 and Ph3CB(C6F5)4 (TIBA/B). The catalyst system sho...

Ethylene-propylene-diene terpolymer (EPDM) having 5-ethylidene-2-norbornene (ENB) as a diene unit was pyrolyzed and the pyrolysis products were analyzed using gas chromatography/mass spectrometry (GC/MS) to develop a method for identification and quantitation of ENB. Pyrolysis products formed fr...

Dinuclear complexes of palladium(II), containing two bridging halogen (Cl or Br) ligands, [NnBu4]2[(X5C6)2Pd(μ-Cl)2Pd(C6X5)2] and [(X5C6)(L)Pd(μ-Y)2Pd(C6X5)(L)] (X = F, Cl; Y = Cl, Br), readily react with cyclopentadienylthallium, C5H5Tl, to give the corresponding air stable half-sandwich, pse...

Self-healing polymer composites based on ring-opening metathesis polymerization (ROMP) incorporating second generation Hoveyda-Grubbs’ (HG2) catalyst as polymerization initiator and 5-ethylidene-2-norbornene (5E2N) as healing monomer are promising for self-healing applications. This is particul...

Three stereoisomers of a wax ester meromycolate have been prepared starting from mannitol. A detailed comparison of their NMR spectra with those reported for a homologous series of natural wax esters allows the relative configurations of the α-methyl group and adjacent trans-cyclopropane to be ...

The syntheses of a number of methoxy and keto-mycolic acids containing an α-methyl-trans-cyclopropane unit and with chain lengths identical to those reported in major homologues in natural samples are reported.

99mTc-exametazime (99mTc-d,l-HMPAO, 99mTc-d,l-hexamethylpropyleneamine oxime) is a neutral rather unstable complex of short-lived 99mTc (t1/2=6 h) with the d,l-isomer (mixture of d,d- and l,l-isomers) of a bis-amine bis-oxime tetraligand. It is widely used for measurement of regional cerebral pe...

c-Met was emerging as an attractive target for cancer-targeted therapy because deregulation of c-Met has been observed in multiple tumor types. A series of 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine derivatives were designed, synthesized and evaluated for their enzymatic inhibitory activity a...

Novel 7-hydrazino-1-ethyl-6,8-difluoroquinolone-3-carboxylate derivatives are obtained by thermochemical reaction of 7-azido-1-ethyl-6,8-difluoroquinolone-3-carboxylate with heterocyclic amines. These new fluoroquinolone carboxylates could be used as precursors in the preparation of novel fluoro...

Cell lines of human glioma (U-343 MGa and U-251 MG) and human glia (U-533 CG) origin were cultured as monolayers and exposed to CV-6209, an alkyl-phospholipid analog and antagonist of platelet activating factor. This drug had very potent antiproliferative effects on the studied human glioma cell...

The reaction of NPBDP with various guanidines affords, after formic acid hydrolysis, 2-amino-5-hydroxy-4-pyrimidones. Reaction of NPBDP with o-aminoheterocycles gives similar results. NPBDP is readily converted to the 3-amino-2-alkenenitrile, 10, a key building block for the synthesis of 5,6-bih...

The acid catalyzed domino reaction of β-nitrostyrenes with methyl 2-(benzo[b][1,4]thiazin-3-ylidene)acetate, which were previously prepared from the cyclization of 2-aminobenzenethiol and methyl 4-chloroacetoacetate, resulted in 2-arylbenzo[b]pyrrolo[1,2-d][1,4]thiazine-3-carboxylates in high y...

The asymmetric syntheses of (R)-(+)- and (S)-(−)-O-methylbharatamine were performed using the lateral metallation strategy, in which (R)- and (S)-phenylalaninol were applied as chiral auxiliaries. The addition reaction of chiral o-toluamide carbanion to 6,7-dimethoxy-3,4-dihydroisoquinoline proc...