Fatty acid binding protein 4 (FABP4) and fatty acid binding 5 (FABP5) are mainly expressed in adipocytes and/or macrophages and play essential roles in energy metabolism and inflammation. When FABP4 function is diminished, FABP5 expression is highly increased possibly as a functional compensatio...

Reactions of 3-[(E)-(dimethylamino)methylidene]-(+)-camphor and (1R,5S)-4-[(E)-(dimethylamino)methylidene]-1,8,8-trimethyl-2-oxabicyclo[3.2.1]octan-3-one with hydrazine derivatives were studied. Treatment of 3-[(E)-(dimethylamino)methylidene]-(+)-camphor with hydrazines afforded the correspondin...

The intravenous injection of methyl methanesulfonate (20–68 mg/kg) in BD IX rats on the 15th and 21st day of gestation led to the development of malignant neurogenic tumours in approximately 20% of the offspring. Two tumours were located in the cerebral hemispheres (classified as oligodendrogli...

Ethane dimethanesulfonate (EDS), a Leydig cell toxicant which results in transient infertility, was used in a 4 day postexposure experimetal protocol designed to identify any effects this compound might exert on the epididymis. The techniques of efferent duct ligation and testosterone (T) implan...

Serious contamination problems are encountered when measuring organic acids in polar ice. Using an involved experimental protocol, methanesulfonate, formate and acetate have been investigated in ice core sections from Antarctica. With CH3SO3− concentrations of a few ppb, HCOO−at a few tenths of ...

Based on a production accident Viracept (nelfinavir mesilate) tablets, an HIV protease inhibitor supplied by Roche outside the US, Canada and Japan was contaminated with relatively high levels of ethyl methanesulfonate (EMS) for at most 3 months in spring of 2007. On the basis of a wide variety ...

Brominated flame retardants (BFRs) represent a large group of chemicals used in a variety of household and commercial products to prevent fire propagation. The environmental persistence and toxicity of some of the most widely used BFRs has resulted in a progressive ban worldwide and the developm...

Synergisms among methyl methanesulfonate (MMS), ethyl methanesulfonate (EMS) and X-rays in inducing somatic mutations were examined in the stamen hairs of Tradescantia clone BNL 4430, a blue-pink heterozygote. The young inflorescence-bearing shoots with roots cultivated in the nutrient solution ...

To improve our understanding of the mechanisms of particulate sulfur formation (non sea-salt sulfate, nss-SO42−) and methanesulfonate (MSx used here to represent the sum of gaseous methanesulfonic acid, MSA, and particulate methanesulfonate, MS−) in the eastern Mediterranean and to evaluate the ...

The pyrazole complexes [ReCl2{N2C(O)Ph}(Hpz)(PPh3)2] 2 (Hpz = pyrazole), [ReCl2{N2C(O)Ph}(Hpz)2(PPh3)] 3 and [ReClF{N2C(O)Ph}(Hpz)2(PPh3)] 4, and the tris(pyrazolyl)methane compounds [ReCl2(HCpz3)(PPh3)][BF4] 5 (pz = pyrazolyl), [ReCl3{HC(pz)3}] 7, [ReOCl2{SO3C(pz)3}(PPh3)] 8 and [ReO3{SO3C(pz)3...

ABSTRACT:Interaction of colistin and colistin methanesulfonate (CMS) with liposomes has been studied with the view to understanding the limitations to the use of liposomes as a more effective delivery system for pulmonary inhalation of this important class of antibiotic. Thus, in this study, lip...

An iron porphycene, a structural isomer of iron porphyrin, with trifluromethyl groups at the peripheral position of the framework was incorporated into sperm whale apomyoglobin. The prepared myoglobin shows the higher O2 affinity than the native protein. However, the oxygen affinity of the recon...

The strategy of searching for highly electrophilic agents in a class of chemically inert compounds – methylenequinone imines – was developed and successfully performed. The first representative of such electrophiles – N-acyl-α-methoxycarbonyl-α-trifluoromethyl-p-methylenequinone imine 6 – ...

The antimicrobial effects of 30 trifluoromethyl ketones [1–30] were studied on various representative bacteria. Of the ketones, 4,4,4-trifluoro-1-phenyl-1,3-butanedione [10], 1,1,1-trifluoro-3-(4,5-dimethyloxazol-2-yl)-2-propanone [11] and 1-(2-benzoxazolyl)-3,3,3-trifluoro-2-propanone [18] wer...

A series of 2-(trifluoromethyl)-1H-benzimidazole derivatives (1a–1i) were synthesized via Phillips cyclocondensation of a substituted 1,2-phenylenediamine and trifluoroacetic acid. The synthesized compounds were evaluated in vitro against various protozoan parasites: Giardia intestinalis, Entam...

The synthesis of several halogenated benzimidazoles substituted in position 2 with trifluoromethyl, pentafluoroethyl and 2-thioethylaminodimethyl group is reported. Antiprotozoal and anticancer activity of series of newly synthesized and previously obtained compounds was studied. All of tested b...

Fluoroform is a potent greenhouse gas which should not be released to the atmosphere. Large amounts of it are stored and wait for new and useful reactions to be based on it. One such general reaction that is described in this paper is its use in preparation of the important organic trifluorometh...

The molecular interactions of 5,6-dichloro-2-(trifluoromethyl)-1H-benzimidazole (G2), an antiprotozoa with poor aqueous solubility, with 2-hydroxypropyl-α-cyclodextrin (HPαCD), methyl-β-cyclodextrin (MβCD) and 2-hydroxypropyl-β-cyclodextrin (HPβCD) were examined. The aqueous solubility enh...

Two new series of C-nucleosidic ATP mimics have been synthesized using an efficient and versatile synthetic pathway. These compounds were designed as FGFR3 inhibitors using purine as a central scaffold. The two substituents, a polyhydroxylated ribose mimic and a lipophilic moiety, were linked ei...

Herein we report both linear and convergent pathways for the preparation of 2-alkynyl substituted adenosine-5′-N-ethylcarboxamides via the versatile synthetic intermediate, 2-iodoadenosine-5′-N-ethylcarboxamide (13). The linear approach afforded 13 in an overall yield of 30% from guanosine ove...