The geometries and energies of polymethyl-1,3-dioxanes were studied by molecular mechanics calculations. Buttressing effects of the Me groups are discussed. The chair/twist conformational equilibrium of 1,3-dioxanes having two syn-axial Me groups in the chair were calculated, and a twist form (t...

A series of new carboxamide and propanamide derivatives bearing phenylpyridazine as a core ring were designed, synthesized and evaluated for their ability to inhibit both cholinesterase enzymes. In addition, a series of carboxamide and propanamide derivatives bearing biphenyl instead of phenylpy...

Fatty acid amide hydrolase (FAAH) has a key role in the control of the cannabinoid signaling, through the hydrolysis of the endocannabinoids anandamide and in some tissues 2-arachidonoylglycerol. FAAH inhibition represents a promising strategy to activate the cannabinoid system, since it does no...

Co(II), Pb(II), Hg(II) and Cd(II) complexes of the 3-(2-(4-(dimethylamino)benzylidene)hydrazinyl)-3-oxo-N-(thiazol-2-yl)propanamide (H2L) were synthesized. The prepared compounds were interpreted by elemental analysis: C, H, N, M, Cl; physical measurements as molar conductance; and magnetic susc...

We evaluated the renal vascular effects of serotonin in Nω-Nitro-l-arginine-hypertensive rats (L-NAME, 30 mg/kg/day, administered over 21 days in drinking water), a model of systemic hypertension with glomerular capillary hypertension and renal disease due to chronic blockade of endogenous synt...

A small library of 3-(5-imidazo[2,1-b]thiazolylmethylene)-2-indolinones has been synthesized and screened according to protocols available at the National Cancer Institute (NCI). Some derivatives were potent antiproliferative agents, showing GI50 values in the nanomolar range. Remarkably, when m...

Monoamine oxidase B (MAO-B) is a promising target for the treatment of neurodegenerative disorders. We report the synthesis and the biological evaluation of halogenated derivatives of 1-aryliden-2-(4-phenylthiazol-2-yl)hydrazines. The fluorinated series shows interesting activity and great selec...

A series of 2-bromo-l-hydroxyquinolizinium bromide substituted anilinium salts have been prepared by reaction of 1-acetoxy-2-bromoquinolizinium bromide with an appropriately substituted aniline. The resulting anilinium derivatives exhibited a moderate to high degree of anti-inflammatory activity...

A series of new 2-substituted [4-(1,3,4-oxadiazol-2-yl)methyl]phthalazin-1(2H)-one derivatives 7a–h to 9a–h were designed and synthesized from methyl (4-oxo-3,4-dihydrophthalazin-1-yl)acetate (4), which in was turn prepared from phthalic anhydride. The structure of synthesized new compounds we...

Novel positive allosteric modulators of sigma-1 receptor represented by 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide enantiomers were synthesised using an asymmetric Michael addition of 2-nitroprop-1-enylbenzene to diethyl malonate. Following the chromatographic separation of the methyl ...

In this study, we employed an efficient strategy by the combinations of chain-growth condensation polymerization (CGCP), styrenics-assisted atom transfer radical coupling (SA ATRC), and ring-opening polymerization (ROP) to synthesize novel miktoarm (μ) star copolymers. Accordingly, poly(N-octyl...

The mechanism of action of benzoin as a degassing agent in powder coatings has been analyzed. The gas bubble shrinkage was monitored using a light microscope equipped with a hot stage. In the absence of benzoin, the air bubbles start to shrink very slowly as a result of a diffusion-controlled pr...

Kinase irregularity has been correlated with several complex neurodegenerative tauopathies. Development of selective inhibitors of these kinases might afford promising anti-tauopathy therapies. While DAPK1 inhibitors halt the formation of tau aggregates and counteract neuronal death, CSF1R inhib...

We have recently shown that the tripeptide l-pyroglutamyl-lhistidyl-l-proline-amide (mammalian TRH) stimulates α-MSH secretion in amphibia. Using a perifusion system technique, we have compared the stereochemical requirements for hormone-receptor interaction of frog melanotrophs with mammalian ...

Publisher SummaryThyrotropin releasing factor (TRF) is a tripeptide the synthesis that can be readily accomplished by peptide chemists. This is emphasized by the large number of reports describing such synthesis. Two general methods—classic synthesis as opposed to solid phase synthesis—can be ...

N-Octanoylglyoxylic amides have been synthesized from N-octanoylisatins and their self-assembly analyzed in the solid state by X-ray crystallography. Of the seven compounds, only two utilize intramolecular N1–H1⋯O2 hydrogen bonds, whereas five of them forgo this intramolecular hydrogen bond to ...

The insect enzyme GH20 β-N-acetyl-d-hexosaminidase OfHex1 represents an important chitinolytic enzyme found in the agricultural pest Ostrinia furnacalis (Guenée) and inhibition of this enzyme has been considered a promising strategy for the development of eco-friendly pesticides. In this artic...

Applications of phase transfer catalysts in etherification reaction of benzyl chloride with furfuryl alcohol in the L-L-L tri-phasic system was investigated. Comparison between the L-L bi-phase system and L-L-L tri-phase system was studied to achieve significant conversion, better selectivity, a...

The complexes of cobalt, copper and nickel ions with the known tridentate ligand 2-(2′-pyridyl)-8-hydroxyquinoline (HQP) were prepared and characterized. The structures of the complexes with Co(II), Cu(II) and Ni(III) were corroborated by crystal structure analyses. The structures of the comple...

Organic compounds derived from 9,10-anthraquinone has attracted a great deal of interest in recent years because of their optical and photosemiconducting properties. In the present paper, 1-(2-methoxy benzyloxy)-8-hydroxy-9,10-anthraquinone compound has been synthesized and films grown by hot wa...