In addition to the psychoactive constituents that are typically associated with Cannabis sativa L., there exist numerous other specialized metabolites in this plant that are believed to contribute to its medicinal versatility. This study focused on two such compounds, known as cannflavin A and c...

Cardiac membranes pretreated with SAdenosylL[methyl-3H] methionine([3H] SAM) purified on TLC silica gel 60 F254 plates exhibited a marked decrease in cyclic AMP and cyclic GMP phosphodiesterase activity. However, this inhibition did not appear when membranes were incubated with either [14C...

In the second part of this two-part review (for Part 1 see V.A. Mamedov, A. Nataliya, N.A. Zhukova, Prog. Heterocycl. Chem. 2012, 24, 55), recent advances in the synthesis of quinoxalines are reviewed. Syntheses that start from pyrazine fragments and from benzenoid units are discussed. The revie...

A practical, convenient, and safe cyano(nitro)methylation method was developed, in which cyano-aci-nitroacetate served as a synthetic equivalent of anionic nitroacetonitrile. A control of the single/double Michael additions was achieved, which enabled the synthesis of unsymmetrical double Michae...

Reaction of 3-nitroisoxazoline-2-oxide with monosubstituted ethenes, first time documented fifty years ago, have been reviewed. Structures of phenyl and cyano derivatives of 1-aza-2,8-dioxabicyclo[3.3.0]octane produced in [3 + 2] cycloaddition (32CA) between styrene and acrylonitrile with 3-nitr...

In the present study, we characterized OXSI-2 [3-(1-Methyl-1H-indol-3-yl-methylene)-2-oxo-2, 3-dihydro-1H-indole-5-sulfonamide], a putative inhibitor of Syk, and determined its specificity and selectivity in platelets. We found that OXSI-2 completely abolished convulxin-induced platelet function...

Synthesis of 2-((1H-indol-3-yl)(aryl)methyl)malononitrile via the Michael addition of indole with various arylmethylenemalononitriles was carried out in good yields using anhydrous zinc chloride as the catalyst under ultrasound irradiation.

Computational studies have been carried out on 3-hydroxy-3-(2-methyl-1H-indol-3-yl) indolin-2-one (HMI) using both the DFT-B3LYP/6-311+G and HF/6-311+G methods. The optimized geometry of HMI and its bonding parameters as well as IR spectra have been calculated and analyzed. It can be seen that t...

An attempt was made to elucidate the relationship between chemical structure, in terms of glass transition temperature (Tg), and conversion temperature (TTR) of thermally rearranged polybenzoxazole membranes, by analyzing DSC and TGA data for a total of 15 sets of o-hydroxypolyimides and copolyi...

We describe a novel experimental method that mimics exposure to dried agrochemical residues on contact surfaces during re-entry into crops. It includes the creation of dry dislodgeable residues and subsequent transfer to human skin for in vitro measurement of dermal absorption within a standard ...

The pyridine scaffold and its benzo derivatives are present in a number of natural products, biologically active materials, as well as in materials with interesting physical and chemical properties. Descriptions of their preparation and application as ligands, solvents, and catalysts increase ea...

Alzheimer's disease (AD) is a neurodegenerative disease which has a higher prevalence and incidence in older people. The need for improved AD therapies is unmet. The 5-hydroxytryptamine4 receptor (5-HT4R) partial agonists may be of benefit for both the symptomatic and disease-modifying trea...

The radical addition of xanthates to Boc-protected azetine gives adducts, which can be reductively dexanthylated to furnish variously substituted azetidines. In the case of α-xanthyl ketones, treatment of the initial adducts with ammonia or primary amines, furnishes 2,4-disubstituted, 2,3,4-tri...

This review covers all aspects of the chemistry of metal complexes of tridentate κ3-N pyridine–pyrrolide ligands, from the syntheses of the ligands to what is known about the metal complexes – their structural and physical properties, and their reactivities, including use in catalytic process...

We report a design strategy to obtain potent DPP-4 inhibitors by incorporating salt bridge formation with Lys554 in the S1′ pocket. By applying the strategy to the previously identified templates, quinoline 4 and pyridines 16a, 16b, and 17 have been identified as subnanomolar or nanomolar inhib...

A new N-oxide was produced from 3-(N-Boc-aminomethyl)-5-bromopyridine by bioconversion with Cunninghamella echinulata var. elegans ATCC 9245, and its structure was established based on the spectral data. The microbial N-oxidation is efficient and highly selective. The substrate was transformed i...

A new series of beta amino acids, which act as CXCR3 antagonists, has been identified. The formerly optimized N,N-disubstituted benzylamine derivatives with carboxylic acid function on the N-atom was used as starting point and compounds with carboxyl function not attached to the N-atom were inve...

The influences of four types of dilute acid washing (H2SO4, HCl, HF, HNO3) on moso bamboo pyrolysis were investigated via pyrolysis–gas chromatography/mass spectrometry (Py–GC/MS). The effects of acid washings on the inorganics contents and the chemical structure were also analyzed. The result...

Phenolic compounds in foods have been widely studied due to their health benefits. In cereals, phenolic compounds are extensively linked to cell wall polysaccharides, mainly arabinoxylans, which cross-link with each other and with other cell wall components. In maize, ferulic acid is the phenoli...

The free fatty acid receptor 1 (FFA1) enhances the glucose-stimulated insulin secretion without the risk of hypoglycemia. However, most of FFA1 agonists have a common biphenyl moiety, leading to a relative deprivation in structure types. Herein, we describe the exploration of non-biphenyl scaffo...