The structural parameters of 1-hexadecyl-3-methylimidazolium chloride (C16MImCl) were computed using B3LYP level of density functional theory. Presence of water of hydration was theoretically studied and rationalized using TG and FTIR heating experiments. Conformation analysis using Raman spectr...

A novel series of 2-phenylquinoline-4-carboxamide derivatives was synthesized, characterized and evaluated for its antiproliferative activity against five cancer cell lines, Hela, SK-OV-3, HCT116, A549 and MDA-MB-468, and a normal human fetal lung fibroblastic cell line, MRC-5. Among them, compo...

In this paper, attempts were made to develop an in situ product removal process for magnesium lactate production based on crystallization. The crystallization was conducted at 42 °C without seed crystal addition. The product concentration, productivity and yield of fermentation coupled with in ...

Ethnopharmacological relevanceAcanthopanax koreanum (Araliaceae) has been used in traditional medicine for enhancing vitality, rheumatism, and bone-related pains. But its activity on cartilage protection has not been known yet.

Stereoselective synthesis of the complete family of optically active dideoxygenated nucleosides of the apiose family have been developed. The chiral aldodiol system 7, a key intermediate in this synthesis, was prepared from the prochiral molecule 6, through the action of the lipase from Candida ...

The radiopacities of seven posterior composite resins, seven composite resin luting cements, and six glass ionomer lining cements were studied. The purpose was to obtain an indication of radiopacity values of different brands within each of these three groups of materials and to show differences...

Contribution of inward rectifier K+ currents (IK1) and ATP-sensitive K+ currents (IKATP) to membrane potential changes of ventricular myocytes appearing during hypotonic challenge is unclear. We used here the whole cell patch clamp technique, voltage and current clamp modes, to record membrane p...

Recent results have shown that the sulfonylurea receptor couples to several types of inward-rectifier potassium (KIR) channels, which suggests that sensitivity to blockade of a pathophysiological phenomenon such as ischemic preconditioning (PC) by glibenclamide may not be the result of this comp...

The maximal responses (Emaxs) of isolated rat gastric fundus strips to 300 nm porcine galanin (Gal) were decreased in a concentration-dependent manner by terikalant (RP 62719). EC50of the agent equalled 4.39 μm (2.35–8.22). On the contrary the action of 30 n m of carbachol were not affected by...

The proarrhythmic activities of the selective IKr blocker erythromycin and the less selective K+ channel blockers, terikalant and clofilium, have been compared in an α1-adrenoceptor-stimulated, anaesthetized rabbit model. Terikalant (2.5, 7.5 and 25 nmol kg−1 min−1; n=10), erythromycin (133, 40...

The cellular mechanism of action of terikalant, an investigational antiarrhythmic agent known to block the inward rectifier and other potassium currents, has not yet been fully clarified. The aim of the present study was therefore to analyse the in vitro electrophysiological effects of terikalan...

Publisher SummaryThis chapter discusses the chemical and biological aspects of sparsomycin, an antibiotic from streptomyces. Sparsomycin is a strong inhibitor of protein biosynthesis, its site of interaction being the large ribosomal subunit, which prevents peptide transfer by interfering with t...

Sparsomycin interaction with the ribosome and characteristics of the drug binding site in the particle were studied using chemical modification of the drug, affinity labeling methods and isolation of drug resistant mutants. The structure-function relationship studies, performed with a large numb...

Propolis, a honey bee hive product, is thought to exhibit a broad spectrum of activities including antibiotic, antiviral, anti-inflammatory and tumor growth inhibition; some of the observed biological activities may be due to caffeic acid (cinnamic acid) esters that are present in propolis. In t...

The nove 3-methyl-3-butenyl, 2-methyl-2-butenyl, 3-methyl-2-butenyl and 2-phenylethyl esters of 3-acetyloxycaffeic acid and 4-acetyloxycaffeic acid were synthesised on a micro scale and characterised by gas chromatography—mass spectrometry. These compounds are identified for the first tiem in p...

The K-region oxides and imines of chrysene, benzo[c]phenanthrene and benzo[g]chrysene were investigated for mutagenicity in Salmonella typhimurium TA98 and TA100, using two different exposure media. All six compounds were mutagenic under all four experimental conditions. The imines were 17–3800...

The synthesis of novel functionalized 3-amino-N-methylfuro[3,2-b]pyridine-2-carboxamides is described from cyanopyridine intermediates. Based on the difference in halogen reactivity, ethyl [(5-bromo-2-chloropyridin-3-yl)oxy]acetate was functionalized by a palladium-catalyzed reaction, before the...

The ring deprotonation of 2-(2- and 4-pyridyl)benzoic acids using lithium dialkylamides in THF at rt, and the in situ cyclization afforded 4- and 2-azafluorenones, respectively. 1-Azafluorenone was obtained from ethyl 2-(3-pyridyl)benzoate using a similar protocol.

Various aromatic bromides were treated with n-BuLi and subsequently with ethyl formate, followed by the reaction with ethanol and molecular iodine in the presence of K2CO3 to provide the corresponding aromatic ethyl esters in good yields. Moreover, aromatic bromides could be transformed into the...

Fifteen new substituted N-2-(2-oxo-3-phenylquinoxalin-1(2H)-yl) acetamides 5a-f, 6a-f, and 8a-c were synthesized by reacting ethyl 2-(2-oxo-3-phenylquinoxalin-1(2H)-yl)acetate with various primary amines including benzylamines, sulfonamides, and amino acids. The in vitro antimicrobial screening ...