To synthesize 4-chloro-5-methoxy-2-(b-trifluoroethyl)-3(2H)-pyridazinone (4), the reactions of 4-chloro-5-methoxy-3(2H)-pyridazinone (5) with RCH(2)CF(3)(R = I, TsO, MsO, TfO) in different solvents were studied. It was found that methyl group migration took place during this reaction. An oxonium salt 9 was suggested as the active intermediate for the formation of the byproduct 4-chloro-5-methox...

The preparation, purification, and analysis of a variety of new sulfonium derivatives of methionine is reported. Deamination of S-adenosyl-L-methionine with nitrous acid yielded, depending on experimental conditions, S-adenosyl L-(Z-hydroxy-4-methylthio)butyric acid or S-inosyl-L-(Z-hydroxy 4 methylthio)butyric acid. S-Inosyl L methionine was obtained by enzymatic deamination of S-adenosyl-Lhom...

Compounds formed by exchanging one of the resveratrol hydroxy groups to methoxy or formyl groups are biologically important. Quantum chemical DFT calculations were applied for the simulation of some of their properties. Their optimized structures and charge distributions were computed. Based on the calculated vibrational force constants and optimized molecular structure infrared and Raman spect...

Abstarct: A series of some new pyrimidine derivatives were synthesized via the reaction of ethyl cyanoacetate with thiourea and the appropriate aldehydes namely 2-methyl-benzaldehyde and 2-methoxy-benzaldehyde to give 1a,b. Compounds 1a,b were chlorinated to give the chloro compounds 2a,b then condensation of 2a,b via different reagents gave compounds 3-5. Compound 4b reacted with acetic anhydr...

LLC-PK1 cells have been stably transfected with cDNAs encoding the human norepinephrine transporter (NET), rat dopamine transporter (DAT), and rat serotonin transporter. Using these cell lines, the specificity of each transporter toward agents that inhibit substrate influx and stimulate substrate efflux across the plasma membrane was examined. With 1-methyl-4-phenylpyridinium as a substrate for...

A series of new thiosemicarbazones derived from natural diterpene kaurenoic acid were synthesized and tested against the epimastigote forms of Trypanosoma cruzi to evaluate their antitrypanosomal potential. Seven of the synthesized thiosemicarbazones were more active than kaurenoic acid with IC₅₀ values between 2-24.0 mM. The o-nitro-benzaldehyde-thiosemicarbazone derivative was the most active...

We present the preparation of tert-butyldiphenylsilanes differing in one functional group. The molecular structures phenyl (3), methoxy (4), and amino derivatives (5) were elucidated by single-crystal X-ray diffraction analysis their crystal packing investigated Hirshfeld surface along with 2D fingerprint plots. In all-C derivative 3, high symmetry dependence enables a multitude directional C(m...

A series of quinoline derivatives was synthesized and biologically evaluated as Enhancer of Zeste Homologue 2 (EZH2) inhibitors. Structure-activity relationship (SAR) studies led to the discovery of 5-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinolin-4-amine (5k), which displayed an IC50 value of 1.2 μM against EZH2, decreased global H3K27me3 level in cells and also show...

Benzotriazole corrosion inhibitors are not completely removed during wastewater treatment and are frequently detected in surface waters. Here, the photochemical kinetics of benzotriazoles and structurally related compounds were assessed for natural aqueous environments. The direct photochemical half-lives during exposure to simulated sunlight ranged from 1.3 to 1.8 days for benzotriazole and it...

Copper(II) complexes 1(2+)-6 of a series of tripodal ligands involving a N3O donor set, namely 2-[(bis-pyridin-2-ylmethyl-amino)-methyl]-4-methoxy-phenol (1L), 2-tert-butyl-4-methoxy-6-[bis-pyridin-2-ylmethyl-amino)-methyl]-phenol (2L), 2-tert-butyl-4-methoxy-6-{[(2-pyridin-2-yl-ethyl)-pyridin-2-ylmethyl-amino]-methyl}-phenol (3L), 2-tert-butyl-4-methoxy-6-{[(6-methyl-pyridin-2-ylmethyl)-pyridi...