Genistein derivatives were synthesized from genistein through a facile sonochemical approach in high yields. The bioassay was performed on ovariectomized (OVX) rats in terms of bone mineral density (BMD) and the weight of bone ash (WBA) to lead to the discovery of eight novel genistein-based selective estrogen receptor modulators. Attention to the structure-activity relationship disclosed that ...

All possible monothio analogues of the mono-, di-, and triethoxy homologues of mescaline have been synthesized and pharmacologically evaluated in man. Modifications at the ring position para to the ethylamine chain, either with a sulfur atom, a longer alkyl chain, or both, lead to compounds of high central nervous system activity. The 4-n-propoxy and 4-n-butoxy homologues and their correspondin...

BACKGROUND Aurones are naturally occurring compounds that belong to flavenoids family and have antiplasmodial effects. This study investigated some new aurones derivatives against chloroquine sensitive Plasmodium falciparum. Here we report the synthesis, in vitro antiplasmodial activity and cytotoxic evaluation of 11 compound from derivatives of (Z)-2- benzylidene-4, 6-dimethoxybenzofuran-3(2H)...

In current research, nine basic esters of para-alkoxyphenylcarbamic acid with incorporated 4-(4-fluoro-/3-trifluoromethylphenyl)piperazin-1-yl fragment, 6i-6m and 8f-8i, were screened for their in vitro antimicrobial activity against Candida albicans, Staphylococcus aureus and Escherichia coli, respectively. Taking into account the minimum inhibitory concentration assay (MIC), as the most activ...

A major cause for dental resin composite restoration replacement is secondary caries attributed to Streptococcus mutans. Salivary esterases were shown to degrade resin composites. Hypothesis: S. mutans contain esterase activities that degrade dental resin composites and adhesives. Esterase activities of S. mutans were measured using synthetic substrates. Standardized specimens of resin composit...

A novel phosphodiesterase-5 (PDE-5) inhibitor was found in a natural health food product. The previously unknown sildenafil analogue was isolated using preparative HPLC. The structure of the compound was elucidated using HPLC with diode array detection (DAD), time-of-flight mass spectrometry (TOF/MS), and nuclear magnetic resonance spectroscopy (NMR). An [M + H](+) ion was detected at m/z 505.2...

In the present investigation, the basic esters of meta-alkoxyphenylcarbamic acid bearing variously substituted N-phenylpiperazine fragment were screened for their in vitro antimicrobial activity against Staphylococcus aureus, Escherichia coli and Candida albicans, respectively. The most effective against Escherichia coli was found the compound 6d (MIC=195,3 μg/mL) bearing simultaneously para-fl...

Aerobic biodegradation behaviour of nonylphenol propoxylates was investigated in two tests with different sewage sludge as inocula. The samples containing target compounds were pre-concentrated using dispersive liquid-liquid microextraction and analysed with the use of high performance liquid chromatography with tandem mass spectrometry. Both primary biodegradation and formation of different bi...

Ester prodrugs are commonly used to increase the intestinal absorption of drugs with permeabilitylimited absorption. The high functional activity of este rases in blood and liver allows a rapid bio acti va tion of the prodrug after reaching the sys temic circu lation. However, the increased efficiency of prodrugs to pass the intestinal barrier may be decreased by its rapid esterase-mediated hyd...

Three kinds of UV-curable organically modified silicates have been prepared to be used as protective coatings for optical fibers. The synthesis involves the reaction of the thiol group of 3-mercaptopropyltrimethoxysilane with a C =C bond in one of the acrylic groups of three commercially available aliphatic triacrylates. The methoxysilyl groups of the synthesized diacrylate methoxysilanes were ...