Nineteen surface sediment samples collected from Baiyangdian Lake and its inflowing river (Fuhe River) in North China were analyzed for polybrominated diphenyl ethers (PBDEs) and decabromodiphenylethane (DBDPE). The concentrations of PBDEs and DBDPE in sediments ranged from 5.5 to 300.7 ng/g dry...

Hydroxylated polybrominated diphenyl ethers (OH-PBDEs) and methoxylated polybrominated diphenyl ethers (MeO-PBDEs) are present in the ecosystem of the Baltic Sea. OH-PBDEs are known to be both natural products from marine environments and metabolites of the anthropogenic polybrominated diphenyl ...

Sediment cores from 12 Chinese lakes were analyzed to investigate the historical inputs of polybrominated diphenyl ethers (PBDEs) and decabromodiphenylethane (DBDPE) during the past few decades. Concentrations of ΣPBDE1 (sum of tri- to hepta-BDEs), ΣPBDE2 (sum of nona- to deca-BDEs) and DBDPE ...

A series of novel 6-(6-alkoxy-2-naphthyl)oxoalkanoates and alkanamides were synthesized as inhibitors of inflammation and 5-lipoxygenase. They were evaluated in vivo for anti-inflammatory activity in the established adjuvent arthritis assay in rats and in vitro as inhibitors of 5-lipoxygenase in...

A series of non-nucleoside ethyl 6-hydroxyquinoline-3-carboxylate derivatives were prepared and evaluated in HepG2.2.15 cells. Most compounds inhibited the expression of viral antigens HBsAg or HBeAg at low concentration. Six compounds, 9f3, 12b6, 12f6, 13b2, 13b6, and 13f6, displayed excellent ...

A novel hydrazone, (E)-Ethyl-4-(2-(furan-2-ylmethylene)hydrazinyl)benzoate (EFHB), has been synthesized and characterized by FT-IR, NMR and Mass spectroscopy, and X-ray diffraction; compound crystallized as translucent light yellow thin plates. EFHB was studied for their binding to human serum a...

Sodium tridecafluorohexanesulfinate (1a) and sodium 1-chloro-2,2,2-trifluoroethanesulfinate (1b) were prepared by the treatment of 1-iodo-tridecafluorohexane and 1-bromo-1-chloro-2,2,2-trifluoroethane with sodium dithionite in a water–acetonitrile solution. Prolonged reaction of 1a with allyl b...

The reaction of ethyl 3-(o-trifluoroacetamidoaryl)-1-propargylic esters with ethyl iodoacetate or α-bromoacetophenone in the presence of K2CO3 in DMSO provides a new simple access to 2-acyl- and 2-ethoxycarbonyl-3-alkenyl indoles.

Three-component reactions of 4-hydroxyindole, aldehydes, and malonodinitrile or ethyl cyanoacetate were developed for the first time by using either potassium fluoride or diethylamine as a catalyst, which provided an easy access to 3,4-fused tricyclic indoles in good to excellent yield. The meri...

A highly enantioselective Diels–Alder reaction of 4,4,4-trifluorocrotonaldehyde and dienes was performed with a diarylprolinol silyl ether catalyst. The reaction with cyclopentadiene, 1,3-cyclohexadiene, and 2-substituted 1,3-butadienes yielded the corresponding cycloadducts bearing a trifluoro...

Novel classes of trifluoromethylthiophenes and thiopyrans have been prepared by the reaction of a β-trifluoromethyl β-thioacrolein with different electrophiles, i.e. phenacyl bromide, enones or activated β-chlorovinylpropenes.

As an extension of our previous work on donepezil-based “bio-oxidizable” prodrug approach, two new classes of N-benzylpyridinium donepezil analogues in tetralone B2 and acetophenone B3 series and a new set of indanone derivatives B1 were investigated along with the corresponding dihydropyridin...

This review covers the carbon-nitrogen (C–N) bond forming reactions of pyridines that include both electrophilic as well as nucleophilic substitution reactions. The electrophilic reactions, such as nitration and nitrosation, include both the classical methods and their recent modifications. Nuc...

Purpose: The purpose of this study was to identify the prevalence and distribution of hypoxic tumor cells in spontaneous canine tumors, and to relate these parameters to various tumor and patient characteristics, such as tumor volume, tumor type, or tumor location.Methods and Materials: Hypoxic ...

Purpose: The purpose of this work was to evaluate multiple injections of CCI-103F, a marker of hypoxia, as a method to quantify alterations in tumor hypoxia during irradiation.Methods and Materials: Twelve dogs with spontaneous solid tumors were given intravenous CCI-103F, and tumor biopsies wer...

Purpose: The purposes of this study were to assess sources of variation in the distribution of nitroimidazole-labeled hypoxic cells in canine tumors and to quantify the reliability of estimating overall nitroimidazole-labeled area fraction from biopsies.Methods and Materials: Hypoxic cells were ...

Purpose: Pimonidazole HCl is widely used in immunohistochemical analyses of hypoxia in normal and malignant tissues. The present study investigates oral administration as a means of minimizing invasiveness.Methods and Materials: Twelve dogs with confirmed malignancy received 0.5 g/m2 of pimonida...

8-Cyclopentyl-3-[(E)-3-[131I]iodoprop-2-en-1-yl]-1-propylxanthine (2*) was generated by iododestannylation of the tributyl-stannyl-precursor with [131I]NaI and chloramine T. The radiochemical yield of 2* was 82 ± 4%, and the purity exceeded 98%. The specific activity was 33 ± 19 GBq/μmol. Aff...

Fully quantitative analysis of the adenosine A1 receptor (A1R) in the brain with 11C-MPDX and positron emission tomography is reported. The kinetics is described using a two-tissue three-compartment model, and estimated binding potentials correspond well with the estimates made by Logan plot. Th...

The binding to human serum albumin (HSA) of two drugs which are chemically related to theophylline, 1-methyl-3-pro-pylxanthine (MPX), a new bronchodilator, and 3-propylxanthine (enprofylline), was investigated in vitro using an ultrafiltration method. The binding process involves one class of bi...