The action of the bradycardiac agents, cilobradine (DK-AH269) and zatebradine (UL-FS49), on the cardiac pacemaker current (If) was investigated on short Purkinje fibres from sheep hearts, using the two-microelectrode voltage-clamp technique, and on isolated rabbit sino-atrial cells with the patc...

An efficient method for the preparation of 2,2-diarylvinyl halides from the corresponding 1,1-diarylethylenes has been developed. N-Halosuccinimides (N-bromosuccinimide or N-chlorosuccinimide) were used as the halogenation reagents. The practicability of this method is highlighted by its simple ...

An efficient, mild and very easy method for the synthesis of 2-fluoroalkylated 1,3-benzodioxole derivatives was developed through a double Michael-addition reaction on ethyl 4,4,4-trifluorobut-2-ynoate with corresponding catechols. The procedure does not require the use of expensive supplementar...

The reaction of 2-phenyl-2-(phenylethynyl)-hexamethyltrisilane (1a) with 2,3-dimethylbutadiene in the presence of Ni(cod)2 at 200°C for 20 h gave 1-[2,3-dimethyl-4-(trimethylsilyl)-2-butenyl]-1-phenyl-1-(phenylethynyl)trimethyldisilane and bis[2,3-dimethyl-4- (trimethylsilyl)-2-butenyl]phenyl (...

The cinchona alkaloid-mediated opening of prochiral cyclic anhydrides in the presence of benzyl alcohol leading to optically active hemiesters is described. Structurally diverse anhydrides are converted into their corresponding benzyl monoesters with either enantiomer being obtained with up to 9...

Iodoperidol (IP), an iodinated analogue of the antipsychotic drug haloperiodol, was evaluated as a cerebral blood flow radiopharmaceutical for PET or SPECT. IP was labelled with 131I or 122I (76% β+, t12 = 3.6 min) in >75% radiochemical yield via electrophilic aromatic iododestannylation. [131I...

Results from two clinical pharmacokinetic studies are given. The first study was an observational study in oral contraceptive users who took either a combination of gestodene and ethinyl estradiol (pill A, Femovan) or desogestrel and ethinyl estradiol (pill β, Marvelon). A total of 69 women (39...

The synthesis of two enantiomeric pairs of pyrimidoisoindoles 9a, 9b and 10a, 10b is reported. During a domino ring-closure reaction, followed by cycloreversion, the chirality of diendo-(−)-(1R,2S,3R,4S)-3-aminobicyclo[2.2.1]hept-5-ene-2-carboxamide [(−)-1] was successfully transfered to heteroc...

The vinylogues of furfurylamines, easily available in two steps from furylacroleins (3-(furyl)allylamines), were studied in a tandem N-acylation/intramolecular [4+2] cycloaddition with maleic, pyrocinchonic, and citraconic anhydrides, as well as furylacryloyl and cinnamoyl chlorides. By using a ...

Effect of selected amino acids (glycine, l-histidine, l-cysteine, l-serine, l-tryptophan) and albumin on the spectroscopic properties and photostability of zinc octacarboxyphthalocyanine (ZnPcOC) was explored in the phosphate buffer at a pH of 7.0. The photodegradation of ZnPcOC alone and in the...

We present the study of synthetic pathways to prepare carboxylic acid substituted phthalocyanines from glycolic and lactic acids. Hydroquinone was used as an alternative catalyst for cyclotetramerization reaction of metal free and zinc phthalocyanines, which were characterized by 1H MR spectrosc...

In this study, a new extraction approach based on rotating molecularly imprinted polymer (MIP) disks was developed. The preparation procedure of MIP-disk is simple. Firstly, in order to immobilize MIP onto the surface of polytetrafluoroethylene (PTFE) disk, previous modification and vinylization...

Methyl decanoate, methyl-5-decenoate and methyl-9-decenoate have been widely adopted as biodiesel surrogates for engine simulation. However, these surrogates have relatively short chain length and very different physical properties compared with biodiesel molecules. Additionally, it is difficult...

Biodiesel contains large methyl esters including methyl palmitate (MP), methyl oleate (MO), methyl linoleate (ML), etc. Long alkyl chains and asymmetric structures of these large methyl esters lead to complexity in development of kinetic models. In this paper, surrogate fuels for large methyl es...

This study aimed the investigation of a potential heterogeneous catalyst for the interesterification reaction for soybean biodiesel production. Different types of catalysts (Y Zeolite, MgO, Nb2O5 and mixed oxides) were tested in this work. Ca-Mg-Al mixed oxide with 40% wt. Ca was the more suitab...

Cycloplatam is a novel platinum compound which has shown anti-tumour activity in murine tumour models. In this study, cycloplatam was found to have anti-tumour activity in vitro and in vivo in human tumour models. In 15 cell lines (mainly ovarian), cycloplatam showed similar cytotoxicity as cisp...

A four-step route for the synthesis of 2-methoxyestradiol (5) starting from 17β-estradiol (1) has been achieved with a 51% overall yield. The key step was the ruthenium-catalyzed ortho-C(sp2)-H bond hydroxylation of aryl carbamates. Using dimethyl carbamate as the directing group, [RuCl2(p-cyme...

Keto–enol tautomerism is a key phenomenon which determines the pharmacological activity of compounds possessing the carbonyl group. In the present study we use X-ray analysis, IR spectroscopy as well as quantum chemical calculation to address the keto–enol tautomerism of 4-substituted 3-[1-met...

The ability of highly purified preparations of human monoamine oxidase A and B (MAO A and B) to utilize 1-methyl-4-(1-methylpyrrol-2-yl)-4-piperidinol (MMPP) and its dehydration product 1,2,3,6-tetrahydro-1-methyl-4-(methylpyrrol-2-yl) pyridine (TMMP) as substrates was investigated. The results ...

The crystal and molecular structure of 1-methylpyrrol-2-yl trichloromethyl ketone (PTK) was determined and the C–Cl⋯O halogen bonds were found. Additionally weak C–H⋯O hydrogen bonds exist in this crystal structure. The motifs containing halogen bond and related through translation symmetry ar...