Potassium canrenoate (PC), a competitive aldosterone antagonist previously found to increase tumor incidence in rats and to produce genotoxic effects in in vitro systems, was examined in rats to acquire information on its genotoxic activity in vivo. Intragastric administration of 1/2 LD50 produc...

1-Substituted imidazoles (R = Me, Et, Ph) react (20–25 °C) with phenylcyanoacetylene to afford the 1:2 adducts, (Z)-1-organyl-2-(2,4-dicyano-1,3-diphenyl-1,3-butadienyl)imidazoles, in 10–20% yields, along with the 1:1 adducts, (Z)-1-organyl-2-(2-cyano-1-phenylethenyl)imidazoles.

Aza-Wittig reaction of N-vinylic phosphazenes with α,β-unsaturated aldehydes leads to the formation of 3-azatrienes through a [2+2]-cycloaddition–cycloreversion process. Subsequent, regioselective [4+2]-cycloaddition of 3-azatrienes with pyrrolidinocycloalkanone affords bicyclic dihydropyridi...

2-Bromo-1-arylethylidenemalononitriles react with conjugated thiolatonitriles to give products of regioselective S alkylation that can be subsequently involved in the Thorpe reaction. Resulting enaminoacrylonitriles form pyridine ring under base catalysis yielding thienodipyridines. According to...

2-(2-Phenylethyl) chromones and a 2-(2-phenylethenyl) chromone, were isolated from the ethanolic extract of Chinese eaglewood. Their structures were determined on the basis of extensive analyses of spectroscopic data. Among those, one showed significant neuroprotective activities against both gl...

Various pyridine o-quinodimethane systems were generated via thermal extrusion of sulfur dioxide from 1,3-dihydro-2,2-dioxothieno[3,4-c]pyridine precursors and derivatives functionalised in the 1- or 3-position of the sulfolene ring moiety. Depending on the nature of the peri-substituents on the...

Norartocarpetin, quercetin and naringenin were found to effectively inhibit 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP) formation through trapping its phenylacetaldehyde and form their adducts in roast beef patties. Six adducts [8-C- or 6-C-(E-phenylethenyl) flavonoids] formed between...

α-(2,4-Difluorophenyl)-α-[(1-(2-(2-pyridyl)phenylethenyI)]-1H-1,2,4-triazole-1-ethanol bismesylate (XD405) exhibits exceptional solubility for a triazole antifungal. The solubility of XD405 in water is high (790 mg/ml at pH 1.51). Changes in pH have a dramatic effect on the solubility with val...

Molasses, the main by-product of sugar production, is a well-known source of antioxidants. In this study, sugarcane molasses extract was investigated for its total phenolic content and in vitro antioxidant capacity. The experimental total phenolic content was 101.3 mg of gallic acid equivalent (...

The present study aimed to investigate in detail the changes to 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP) and its precursors in the presence of some cations (i.e., K+, Na+, Ca2+, Mg2+, Fe2+ and Fe3+) in a creatinine/phenylacetaldehyde model system. Results showed that PhIP yields de...

Reaction of conjugated enynones,1,5-diarylpent-2-en-4-yn-1-ones, with malononitrile and sodium alkoxides in the corresponding alcohols at room temperature for 3–23 h results in the formation of two types of compounds (E)-/(Z)-6-aryl-4-(2-arylethenyl)-2-alkoxypyridine-3-carbonitriles (substitute...

A simple and sensitive poly(L-aspartic acid)/electrochemically reduced graphene oxide modified glassy carbon electrode, P(L-Asp)/ERGO/GCE, was constructed by electrochemical reduction of GO drop coated on glassy carbon electrode within 2 mM L-aspartic acid by cyclic voltammetry in pH 6 PBS which...

Hydrophobically modified ethoxylated urethanes (HEURs), as a representative class of associative polymers, are widely used as rheology modifiers in waterborne systems such as coatings, emulsions, inks etc. due to their unique associative network structure and finite relaxation behavior in soluti...

In general, potent non-ketolide versions of erythromycin possessed conformationally constricted two- or three-atom-length sidechains at 3-OH. Novel 14-membered non-ketolides possessing long spacers beyond three-atom length were evaluated for antibacterial activity. The most potent one is 34a, fe...

A series of 2-substituted 6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids was prepared and evaluated for antibacterial activity. The 6-fluoro-2-methyl-1-prenyl-1,4-dihydro-7-(3,5-dimethylpiperazinyl)-4-oxo-3-quinolinecarboxylic acid (14f) exhibited the most potent antibacterial activity a...

We show that a monocationic CpRu(II) complex of quinaldic acid (QAH) and a monocationic CpRu(IV)(π-allyl)QA complex catalyze efficient cleavage of the allyloxy bond in allyl ethers, allyl esters, allyl carbonates, and allyl carbamates in methanol without the need for additional nucleophiles. Th...

Aglafoline, isolated from Aglaia elliptifolia Merr, inhibited in a selective and concentration-dependent manner the aggregation and ATP release reaction induced in washed rabbit platelets by PAF (platelet-activating factor). The IC50 values of aglafoline, BN52021 and kadsurenone on PAF (3.6 nM)-...

The effects of synthetic ω-grammotoxin SIA (ra-GsTx SIA) and synthetic ω-Aga-IVA were tested in in vitro and in vivo neurochemical assays that are reflective of voltage-sensitive calcium channel function. Synthetic ω-GsTx SIA inhibited K+-evoked rat and chick synaptosomal 45Ca2+ flux, K+-evok...

ω-Grammotoxin SIA (GrTx) is a 36 amino acid residue protein toxin from spider venom that inhibits P/Q and N-type voltage-gated Ca2+ channels by modifying voltage-dependent gating. We determined the three-dimensional structure of GrTx using NMR spectroscopy. The toxin adopts an “inhibitor cysti...

ω-Grammotoxin SIA (ω-GsTx SIA), a peptide isolated from tarantula venom, inhibits synaptosomal Ca2+ influx and neurotransmitter release, and blocks N-, P-, and Q-type voltage-gated Ca2+ channels. The whole-cell patch-clamp was used to record glutamatergic excitatory post-synaptic currents (EPS...