Synthesis of pyrazolo[1,5‐a]‐, 1,2,4‐triazolo[1,5‐a]‐ and imidazo[1,2‐a]pyrimidines related to zaleplon,a new drug for the treatment of insomnia

This paper describes the preparation of some pyrazolo[1,5‐a]‐, 1,2,4‐triazolo[1,5‐a]‐ and imidazo[1,2‐a]‐pyrimidines substituted on the pyrimidine moiety by a 4‐[(N‐acetyl‐N‐ethyl)amino]phenyl group. A new synthesis of related benzo[h]pyrazolo[1,5‐a]‐, benzo[h]pyrazolo[5,1‐b]‐ and benzo[h]1,2,4‐triazolo[1,5‐a]‐quinazolines is also reported.     

A comparison result related to Gauss measureUn résultat de comparaison relatif à la mesure de Gauss

In this paper we prove a comparison result for weak solutions to linear elliptic problems of the type

where $\text{Ω}$ is an open set of $\text{R}{}^{\mathrm{n}}$ (n?2), ?(x)=(2π)^?n/2exp(?|x|²/2), a_ij(x) are measurable functions such that a_ij(x)ξ_iξ_j??(x)|ξ|² a.e. $\text{x∈Ω}$, $\text{ξ∈}\text{R}{}^{\mathrm{n}}$ and f(x) is a measurable function taken in order to guarantee the existence of a solution $\text{u∈}\text{H}{}^1{}_0\text{(?,Ω)}$ of (1.1). We use the notion of rearrangement related to Gauss measure to compare u(x) with the solution of a problem of the same type, whose data are defined in a half-space and depend only on one variable. To cite this article: M.F. Betta et al., C. R. Acad. Sci. Paris, Ser. I 334 (2002) 451–456.     

Non-covalent synthesis in aqueous solution of discrete multi-porphyrin aggregates with programmable stoichiometry and sequence

This unprecedented calixarene templated, noncovalent synthesis of multi-porphyrin complexes in aqueous solution makes it possible to plan the nature, stoichiometry, and sequence of porphyrins. The proposed method presents the same accuracy of the covalent approach and a 100% yield, but it is not as time-consuming as the latter method.     

Membraneless vanadium redox fuel cell using laminar flow

This paper describes the design and characterization of a small, membraneless redox fuel cell. The smallest channel dimensions of the cell were 2 mm x 50 mum or x 200 mum; the cell was fabricated in poly(dimethylsiloxane) using soft lithography. This all-vanadium fuel cell took advantage of laminar flow to obviate the need for a membrane to separate the solutions of oxidizing and reducing components.     

PARP Theranostic Auger Emitters Are Cytotoxic in BRCA Mutant Ovarian Cancer and Viable Tumors from Ovarian Cancer Patients Enable Ex-Vivo Screening of Tumor Response

Theranostics are emerging as a pillar of cancer therapy that enable the use of single molecule constructs for diagnostic and therapeutic application. As poly adenosine diphosphate (ADP)-ribose polymerase 1 (PARP-1) is overexpressed in various cancer types, and is localized to the nucleus, PARP-1 can be safely targeted with Auger emitters to induce DNA damage in tumors. Here, we investigated a radioiodinated PARP inhibitor, [¹²⁵I]KX1, and show drug target specific DNA damage and subsequent killing of BRCA1 and non-BRCA mutant ovarian cancer cells at sub-pharmacological concentrations several orders of magnitude lower than traditional PARP inhibitors. Furthermore, we demonstrated that viable tumor tissue from ovarian cancer patients can be used to screen tumor radiosensitivity ex-vivo, enabling the direct assessment of therapeutic efficacy. Finally, we showed tumors can be imaged by single-photon computed tomography (SPECT) with PARP theranostic, [¹²³I]KX1, in a human ovarian cancer xenograft mouse model. These data support the utility of PARP-1 targeted radiopharmaceutical therapy as a theranostic option for PARP-1 overexpressing ovarian cancers.     

Preservation of vitamins content in Cuccìa using an innovative method of processing

Abstract

Cuccìa is a traditional Sicilian food prepared by boiling whole durum wheat kernels, in water, for many hours. This process destroys the vitamins E and B contents of crude kernels. It was rated a method to prepare the Cuccìa, preserving the vitamin content. Four varieties of durum wheat were processed comparing the traditional cooking method (TR-boiling for 5/6?hours), and an innovative one (IN-grains scarification, germination, and cooking at 50?°C for 2?hours). On soups obtained the content of biotin, niacin and α-amylase activity were determined. ANOVA showed the cooking method influences biotin and niacin content having values from 0.56 and 0.72?ng ml^?1 (raw grain) and values close to 0 (TR), while only a 10% decrease (IN) respectively for both vitamins. On the contrary, α-amylase activity was reduced with IN method. The IN method combined with ancient grains, produces the soup with a good vitamin B amount.     

Synthesis of 3-benzoyl-4-benzylfurans structural related to furolignans

Abstract

Furolignan-type natural products, possessing important biological properties, have been synthesized from a commercially available furan. The elaborated synthetic strategy is based on an innovative Friedel-Crafts reaction starting from an alcohol or a carboxylic acid and triflic anhydride as promoter. Through this synthetic strategy, furolignans having two different aryl groups have been obtained. The products have been evaluated for their antimicrobial properties on Gram positive and Gram negative bacteria, in order to compare their biological activities with those of natural analogues.     

A molecularly imprinted polymer for the determination of neopterin

A molecularly imprinted polymer (MIP) for the specific retention of neopterin has been developed. A set of 6 polymers was prepared by radical polymerization under different experimental condition using methacrylic acid as functional monomer and ethylene glycol dimethacrylate as crosslinker, with the aim to understand their influence on the efficiency of the MIP. The performance of each MIP was tested in batch experiments via their binding capacity. The MIP prepared in the presence of nickel ions in dimethylsulfoxide-acetonitrile mixture (P4) exhibited the highest binding capacity for neopterin (260 μmol per gram of polymer). A selectivity study with two other pteridines demonstrated the polymer P4 also to possess the best selectivity.

A molecularly imprinted polymer for the specific retention of neopterin was developed. A set of 6 polymers was prepared under different experimental condition. The performance of each MIP was tested through their binding capacity. The MIP P4 prepared in the presence of nickel ions exhibited the highest binding capacity

     

Photodegradation of Brilliant Green Dye by a Zinc bioMOF and Crystallographic Visualization of Resulting CO2

We present a novel bio-friendly water-stable Zn-based MOF (1), derived from the natural amino acid L-serine, which was able to efficiently photodegrade water solutions of brilliant green dye in only 120 min. The total degradation was followed by UV-Vis spectroscopy and further confirmed by single-crystal X-ray crystallography, revealing the presence of CO₂ within its channels. Reusability studies further demonstrate the structural and performance robustness of 1.