2-[2-(Acetylamino)-4-[bis(2-hydroxyethyl)amino]-5-methoxyphenyl]-5-amino-7-bromo-4-chloro-2H-benzotriazole (PBTA-6) and 4-amino-3,3′-dichloro-5,4′-dinitrobiphenyl (ADDB) are two compounds, which show strong mutagenicity toward bacteria, that have been identified as major mutagens in river wate...

In this paper we report the SAR studies of a series of N-(4-(4-chloro-1H-imidazol-1-yl)-3-methoxyphenyl)amide and N-(4-(4-chloro-1H-imidazol-1-yl)-3-methoxyphenyl)sulfonamide derivatives 6(a–o) and 7(a–o), were synthesized in good yields and characterized by 1H NMR, 13C NMR and mass spectral a...

In this paper we report the synthesis and the chemotaxis inhibitory activity of a number of 1H-pyrazole-4-carboxylic acid ethyl esters 2 functionalized in N1 with a methyl group or different hydroxyalkyl chains and in position 5 with a series of 3-substituted urea groups. These compounds were de...

Malononitriles are valuable synthetic intermediates for many applications, including the synthesis of herbicides and other biologically active molecules, and the synthesis of chiral ligands for asymmetric catalysis. This article describes the development of a procedure for the conversion of prim...

The synthesis of ethyl and methyl esters of 2-substituted 5-cyano-1,6-dihydro-6-oxo-3-pyridinecar☐ylic acids by reaction of ethyl or methyl 2-dimethylaminomethylene-3-oxoalkanoates with sodium cyanoacetamide is described. These esters gave by alkaline hydrolysis the corresponding car☐ylic acids,...

Caesalpinia sappan L. (Lignum Sappan) is a Chinese medicinal plant for treating ischemic cerebral apoplexy. Deoxysappanone B (DSB), a homoisoflavone compound isolated from C. sappan L. (Lignum Sappan), was studied for anti-neuroinflammatory and neuroprotective properties using lipopolysaccharide...

A bioactivation mechanism for myrocin C (1) is offered in which doubly activated spiro cyclopropane 4 emerges as the reactive intermediate. Support for this proposal is found in comparison of the behavior of 1 with that of 6-desoxymyrocin C (6).

We have achieved a synthesis of multiply arylated pyridines by using a [4 + 2] cycloaddition of 2,4-diaryl-5-chloroxazoles and cinnamic acids as a key reaction. The resulting hydroxytriarylpyridines can be derivatized into triarylpyridines, tetraarylpyridines and pentaarylpyridines by sequential...

In this study, a commercial lipase derived from Candida cylindracea was chemically modified with dextran by conjugating ε-amine in the lysine residue with the carbonyl residue in oxidized dextran using the borane-pyridine complex as a reducing agent to increase the hydrophilicity of the microen...

Drug-resistant bacteria associated with biofilm formation are rapidly on the rise, requiring novel therapeutic options to combat biofilm induced drug-resistance. In this study, a class of 3-hydroxy-2-(phenylhydroxy-methyl)-6-methyl-4H-pyran-4-one derivatives (1a-1e) were found by screening of an...

The synthesis and characterization of a novel pyridine coordinated dichloridopalladium(II) NHC complex is described. This compound possesses a saturated NHC ligand that is substituted with a para-nitrophenyl function in the 4-position of the NHC backbone. It is accessible in four steps with over...

In hydroalcoholic medium, electrochemical oxidation of Nifedipine and its N-methyl derivative on one hand and of the analog 3,5-dicyano-2,6-dimethyl-4-(o-nitrophenyl)-1,4-dihydropyridine and its N-methyl derivative on the other leads to the corresponding o-nitrophenyl-pyridines or pyridinium sal...

Chalcone and its derivatives are well-known for their high non-linear optical behavior and charge transfer characteristics. The effectiveness of charge transfer via ethylenic group and increase in NLO response of the chalcone upon substitutions are of great interest. The present study focuses th...

Whereas iodonium ion-induced intramolecular cyclization of 3-butenyldiphenylsilanol proceeded via exo mode cyclization to give 5-iodomethyl-2,2-diphenyl-1-oxa-2-silacyclopentane selectively, iodosilyletherization of 4-methyl-3-pentenyldiphenylsilanol afforded 6,6-dimethyl-5-iodo-2,2-diphenyl-1-o...

Several phenylethyl-substituted pyridinecarboxaldehydes were prepared from 2-bromo-3-pyridine-carboxaldehyde and these substances are found to undergo cyclization reactions in acidic media. In the absence of added nucleophile, acid-promoted cyclization and oxidation (MnO2) provide an efficient r...

Astrocytes, the most common type of glial cell, are critical to the health of the central nervous system. Evidence implies that changes in the astrocyte's cytosolic calcium concentration is part of a central mechanism by which information is passed and processed in the cell, and it is linke...

ObjectivesIn older adults, type-2 diabetes mellitus (T2DM) impacts cognition and increases dementia risk. Prior studies suggest that impaired neuroplasticity may contribute to the cognitive decline in T2DM, but the underlying mechanisms of altered neuroplasticity are unclear. We investigated the...

Glucose inhibits ∼60% of lateral hypothalamic (LH) orexin neurons. Fasting increases the activation of LH orexin glucose-inhibited (GI) neurons in low glucose. Increases in spontaneous glutamate excitatory postsynaptic currents (sEPSCs) onto putative VTA DA neurons in low glucose are orexin dep...

BackgroundGlutamate, glutamine are involved in energy metabolism, and have been related to cardiometabolic disorders. However, their roles in the development of type-2 diabetes (T2D) remain unclear.

SummaryN-acetyl-aspartyl-glutamate (NAAG) is a peptide-based neurotransmitter that has been extensively studied in many neurological diseases. In this study, we show a specific role of NAAG in cancer. We found that NAAG is more abundant in higher grade cancers and is a source of glutamate in can...