Lidia De Luca

Bio: Lidia De Luca is an academic researcher from University of Sassari. The author has contributed to research in topics: Catalysis & Trichloroisocyanuric acid. The author has an hindex of 26, co-authored 103 publications receiving 2403 citations.

Naturally Occurring and Synthetic Imidazoles: Their Chemistry and Their Biological Activities

Abstract: Imidazoles are an important class of heterocycles and include many substances of both biological and chemical interest. They are part of a large number of highly significant biomolecules such as the essential amino acid histidine and related compounds, biotin, and the imidazole alkaloids. Insertion of the imidazole nucleus is an important synthetic strategy in drug discovery. Imidazole drugs have broad applications in many areas of clinical medicine. The imidazoles are a class of antifungal azole derivatives and have a broad spectrum of activities both in vitro and in vivo. The imidazole moiety is also contained in many histaminergic ligands for histamine H1, H2, and H3 receptors. These are currently used as tools in pharmacological studies. The important therapeutic properties of imidazole related drugs have encouraged the medicinal chemists to synthesize and test a large number of novel molecules. Some of these have chemotherapeutic properties, such as for example several FTase inhibitors with an imidazole moiety. Imidazole derivatives have also been shown to have antibacterial activity and recently several P38 MAP Kinase inhibitors and 5-Lipoxygenase inhibitors containing the imidazole moiety have been synthesized. This review reports current progress in the area of new biologically active imidazoles and recently discovered naturally occurring imidazole.

Beckmann Rearrangement of Oximes under Very Mild Conditions

Abstract: A variety of ketoximes, easily prepared from the corresponding ketones, undergo the Beckmann rearrangement upon treatment with 2,4,6-trichloro[1,3,5]triazine in N,N-dimethylformamide at room temperature in excellent yields. This procedure can be applied to aldoximes for obtaining the corresponding nitriles.

Trichloroisocyanuric/TEMPO oxidation of alcohols under mild conditions: a close investigation

Abstract: Efficient oxidation of primary alcohols to the corresponding carboxylic acids can be carried out at room temperature and in acetone/water, using trichloroisocyanuric acid (TCCA) in the presence of catalytic TEMPO. The mild conditions of this procedure and the total absence of any transition metal make this reaction suitable for safe laboratory use. A possible mechanism is presented and discussed.

Metal-Mediated and Metal-Catalyzed Reactions Under Mechanochemical Conditions

Abstract: The extraordinary impact of metal-based complexes on synthetic methods is still recognized nowadays, and attempts are currently undertaken to further extend the use of metal-assisted chemistry to e...

Controlled microwave heating in modern organic synthesis.

Abstract: Although fire is now rarely used in synthetic chemistry, it was not until Robert Bunsen invented the burner in 1855 that the energy from this heat source could be applied to a reaction vessel in a focused manner. The Bunsen burner was later superseded by the isomantle, oil bath, or hot plate as a source for applying heat to a chemical reaction. In the past few years, heating and driving chemical reactions by microwave energy has been an increasingly popular theme in the scientific community. This nonclassical heating technique is slowly moving from a laboratory curiosity to an established technique that is heavily used in both academia and industry. The efficiency of "microwave flash heating" in dramatically reducing reaction times (from days and hours to minutes and seconds) is just one of the many advantages. This Review highlights recent applications of controlled microwave heating in modern organic synthesis, and discusses some of the underlying phenomena and issues involved.

Drug development from marine natural products

Abstract: Drug discovery from marine natural products has enjoyed a renaissance in the past few years. Ziconotide (Prialt; Elan Pharmaceuticals), a peptide originally discovered in a tropical cone snail, was the first marine-derived compound to be approved in the United States in December 2004 for the treatment of pain. Then, in October 2007, trabectedin (Yondelis; PharmaMar) became the first marine anticancer drug to be approved in the European Union. Here, we review the history of drug discovery from marine natural products, and by describing selected examples, we examine the factors that contribute to new discoveries and the difficulties associated with translating marine-derived compounds into clinical trials. Providing an outlook into the future, we also examine the advances that may further expand the promise of drugs from the sea.

A new criterion for the determination of molecular structures from ground state rotational constants

Abstract: Kraitchman has shown that a single isotopic substitution on an atom is sufficient to determine directly the coordinates of that atom with respect to the principal axes of the original molecule. Kraitchman's formulas represent exact solutions of the equations for the equilibrium moments of inertia. However, the effects of the zero‐point vibrations are such that the coordinates obtained by substitution from the ground state moments of inertia I0 are systematically less than r0. These coordinates have here been called r (substitution) or rs, and it is found that rs≃(r0+re)/2, and Is= ∑ imirsi2≃(I0+Ie)/2.In the usual method of solution, the coordinate of one atom is determined from the equation for I0, and therefore the difference I0—Is must be made up by this one coordinate. This introduces a large error in the structures normally determined from ground state constants, and results in variations of 0.01 A in structures determined from different sets of isotopic species. If instead, we obtain the structure on...