Anticancer activity and evaluation of apoptotic genes expression of 2-azetidinones containing anthraquinone moiety

Molecular Diversity - Nowadays, one of the principal causes of death in the world is cancer. A series of 2-azetidinones containing anthraquinone moiety with various substituents were synthesized...     

Aluminium(III)-selective electrode based on a newly synthesized tetradentate Schiff base

A PVC membrane electrode for aluminium ion based on bis(5-phenyl azo salicylaldehyde) 2,3-naphthalene diimine (5PHAZOSALNPHN) as an ion carrier was developed. The electrode exhibits a Nernstian slope of 19.3+/-0.8 mV per decade and a linear range of 5.0x10(-6)-1.0x10(-2) M for Al(NO(3))(3). The limit of detection is 2.5x10(-6) M. It has a fast response time of about 10 s and can be used for at least 10 weeks without observing any deviation. The proposed membrane sensor revealed good selectivity for Al(3+) over a wide variety of other metal ions and could be used in pH range of 2.9-5.0. It was used as an indicator electrode in potentiometric titration of aluminium ion.     

Petra,Osiris, and Molinspiration Together as a Guide in Drug Design: Predictions and Correlation Structure/Antibacterial Activity Relationships of New N-Sulfonyl Monocyclic β-Lactams

We report in this article the design and calculated molecular properties of 18 new mono-cyclic β-lactams 4–21, on the basis of one hypothetical antibacterial pharmacophore structure designed to interact with both of Gram-positive bacteria and Gram-negative bacteria. The in vitro biological evaluation of these compounds allowed us to point out new potential non-nucleoside hits, with MIC values in the range of 2–8 μg/mL active against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Pseudomonas aeruginosa. A correlation structure/antibacterial activities relationship of these monocyclic β-lactams is described.

Supplemental materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the Related Elements to view the free supplemental file.     

Synthesis of β-Lactams from Acids and Imines Using Thiocarbonyldiimidazole

Thiocarbonyldiimidazole has been found to be an efficient acid activator for the synthesis of β-lactams by ketene-imine cycloaddition at room temperature. The experimental procedure is simple and results in excellent yields of the products. All products were characterized by spectral data and elemental analyses.     

Efficient one-pot synthesis of 2-azetidinones from acetic acid derivatives and imines using methoxymethylene-N,N-dimethyliminium salt

A cheap, versatile and convenient method for synthesis of β-lactams using methoxymethylene-N,N-dimethyliminium salt as an acid activator in Staudinger reaction is reported. This method is used for the preparation of monocyclic, spirocyclic, N-alkyl and three-electron-withdrawing group β-lactams. The products are obtained in good to excellent yields.     

Synthesis of ethyl cis 2-[(Diethoxyphosphoryl)methyl]-7-oxo-3-phenyl-6-phthalimido-l-azabicyclo[3.2.0]hept-3-ene-2-carboxylate and Methyl cis-2-Bromo-3-methyl-8-oxo-7-phthalimido-4-oxa-1-azabicyclo[4.2.0]octane-2-carboxylate

The synthesis of a Δ¹-carbapenem and two β-lactams possessing a Br-atom at the N-substituting center not involved in the lactam ring and bearing the carboxyl group is described. The β-lactams having this kind of Br-substitution are more susceptible to nucleophilic attack than those having a conjugated double bond with the N-atom of the β-lactam ring. DBU is found to be an excellent reagent for the elimination of the silyloxy function. Moreover, a simple method for the addition of diethyl phosphite to an α, β-unsaturated double bond using a catalytic amount of NaH is described.     

Homogenized Lorentz-Drude optical response in highly nanoporous conducting gold layers produced by de-alloying

Nanoporous gold films produced by de-alloying AuAl₂ with void densities between 45% and 65% retain high infra-red reflectance and good conductivity. They act optically like a homogeneous Lorentz-Drude metal with a unique plasma frequency and an inter-band transition energy unchanged from that of dense gold. The link between and ω_p in dense gold is found using a simplification of the Bergman expansion for permittivity valid at infra-red wavelengths. The carrier relaxation time of the “effective metal” becomes the actual relaxation time in the Au network and the complex refractive indices (n, k) found using normal incidence spectrophotometry and oblique incidence ellipsometry agree closely with each other. The single pole approximation for the ratio in the infra-red allows estimates of void content and the apparent shift in carrier effective mass. It is then possible to model with no adjustable parameters, the full UV-visible-NIR spectral response, giving excellent agreement with data. A range of films with these properties are presented.     

DMF-dimethyl sulfate as a new reagent for the synthesis of β-lactams

A number of 2-azetidinones were synthesized in good to excellent yields by a novel reaction between Schiff bases, substituted acetic acids and alkoxymethylene-N,N-dimethyliminium salts, the adduct formed from DMF and O-alkylating agents. The advantages of this new method are mild reaction conditions, low cost, avoiding the use of chlorinating agents and easy purification of the products. The best results were obtained when DMF and dimethyl sulfate were used at room temperature.