The condensation of 2-aminoindole-3-carbonitriles and their 3-aminoindole-2-carbonitrile isomers with various DMF-dialkoxyacetals was investigated under microwaves. The appearance of reactive and versatile alkoxyiminium species allowed convenient access to indole precursors of building blocks with potential biological activity. The experimental results have been rationalised using DFT calculati...

The reactions of benzo[e][2,1]thiazine-4-chloro-3-carbaldehydes 1 and benzo[e][2,1]thiazine-4-chloro-3-carbonitriles 2 with a number of oxidizing and reducing agents are reported. A number of new, highly functionalized benzo[e][2,1]thiazine derivatives having potential biological activity were synthesized and described.

The binding of [3H]physalaemin [( 3H]PHY) to rat brain membranes is specific, saturable and reversible in the presence of monovalent cations and peptidase inhibitors. Monovalent cations increase the binding of [3H]PHY in an ionic strength (mu)-dependent manner with an optimal effect at mu higher than 0.3. Addition of 2.5 mM MnCl2 results in a 2-fold increase in the affinity (KD) and a 40% incre...

We investigated platelet 14C-serotonin uptake and platelet [3H]LSD and [3H]paroxetine binding in 11 patients with seasonal affective disorder (SAD). Patients were reinvestigated after light therapy, applied at 07.00-09.00 h for 10 consecutive days. The degree of depression was rated before and after light therapy using the Comprehensive Psychopathological Rating Scale (CPRS). Baseline data in p...

Land subsidence has to be controlled under global climate change and sea level rising for coastal megacities. caused by lowering groundwater during underground excavation become a dominant influence factor land urbanization city renewal. How manage the induced foundation pit dewatering (FPD) on an urban scale was urgent. Shanghai selected as research background. A drawdown double control (SDDC)...

A series of 1,3-benzoxazole-4-carbonitriles was synthesized and evaluated for its antifungal activity, solubility, and metabolic stability. Among those compounds, 4-cyano-N,N,5-trimethyl-7-[(3S)-3-methyl-3-(methylamino)pyrrolidin-1-yl]-6-phenyl-1,3-benzoxazole-2-carboxamide (16b) exhibited potent in vitro activity against Candida species, higher water solubility, and improved metabolic stabilit...

The development of resistance poses a serious problem in the therapy cancer due to necessity multiple-drug and unlimited treatment affected patients. In chronic myeloid leukemia (CML), introduction imatinib has revolutionized therapy. persistence an untreatable stem cell pool other resistance-causing factors, however, also impede cure this malignancy. New therapeutic approaches are therefore es...

Various properties of retinyl ester hydrolysis in the liver and the retinal pigment epithelium (RPE) have been studied, yet the relationship between the retinyl ester hydrolase (REH) activities in these tissues of the same species is not known. In the present study, REH activities in bovine liver and RPE microsomes were compared to explore potential biochemical relationships of retinyl ester me...

A series of new 3-Aryl-4-(4-methoxyphenyl)-1-phenyl-4,5-dihydro-1H-pyrazole-5-carbonitriles (1) were screened in vitro for their antibacterial and antifungal activities against four different organisms. The minimal inhibitory concentration (MIC’s) was determined against each organism. The compounds were tested for their antioxidant activity and reducing power ability. The effect of substitution...