Search results for "combinatorial"
showing 10 items of 1208 documents
A Versatile Approach to CF3-Containing 2-Pyrrolidones by Tandem Michael Addition-Cyclization: Exemplification in the Synthesis of Amidine Class BACE1…
2015
The synthesis of new fluorinated pyrrolidones starting from unprotected amino esters and amino nitriles through a Michael addition-lactamization sequence is described. The resulting CF3 -containing building blocks, bearing a quaternary stereogenic center adjacent to the fluorinated group, have been converted into amino pyrrolidines that display potent β-secretase 1 (BACE1) inhibitory activity. This work constitutes an example of selective fluorination as a valid strategy for the modulation of physicochemical and biological properties of lead compounds in drug discovery.
Highly enantioselective synthesis of fluorinated gamma-amino alcohols through proline-catalyzed cross-Mannich reaction.
2005
A new, simple route for the synthesis of fluorinated beta-alkyl gamma-amino alcohols in optically pure form in only two steps and featuring proline catalysis from inexpensive and readily available starting materials is described. The applied strategy allows for the introduction of diversity into both the beta-fluoroalkyl and alpha-alkyl groups of these compounds. [reaction: see text]
New Cathepsin Inhibitors to Explore the Fluorophilic Properties of the S 2 Pocket of Cathepsin B: Design, Synthesis, and Biological Evaluation
2011
5 páginas, 1 figura, 2 tablas -- PAGS nros. 5256-5260
An efficient synthesis of new fluorinated uracil derivatives.
2003
A series of potentially biologically active fluorinated uracil derivatives has been prepared in three steps from oxazolines and fluorinated nitriles with good chemical yields. Fustero Lardies, Santos, Santos.Fustero@uv.es ; Sanz Cervera, Juan Francisco, Juan.F.Sanz@uv.es ; Asensio Martinez, Amparo, Amparo.Asensio@uv.es
New folate-functionalized biocompatible block copolymer micelles as potential anti-cancer drug delivery systems
2006
Abstract The main objective of this study was to synthesize novel folic acid-functionalized diblock copolymer micelles and evaluate their solubilization of two poorly water-soluble anti-tumor drugs, tamoxifen and paclitaxel, which suffer from low water solubility and/or poor hydrolytic stability. The diblock copolymer consisted of a permanently hydrophilic block comprising 2-(methacryloyloxy)ethyl phosphorylcholine (MPC) residues and a pH-sensitive hydrophobic block comprising 2-(diisopropylamino)ethyl methacrylate (DPA) residues. Folic acid (FA) was conjugated to the end of the MPC block so that this group was located on the micelle periphery. Tamoxifen- and paclitaxel-loaded micelles were…
Inulin-based polymer coated SPIONs as potential drug delivery systems for targeted cancer therapy
2014
This paper deal with the synthesis and characterization of PEGylated squalene-grafted-inulin amphiphile capable of self-assembling and self-organizing into nanocarriers once placed in aqueous media. It was exploited as coating agent for obtaining doxorubicin loaded superparamagnetic iron oxide nanoparticles (SPIONs) endowed with stealth like behavior and excellent physicochemical stability. Inulin was firstly modified in the side chain with primary amine groups, followed in turn by conjugation with squalenoyl derivatives through common amidic coupling agents and PEGylation by imine linkage. Polymer coated SPIONs were so obtained by spontaneous self-assembling of inulin copolymer onto magnet…
Combined study of anion recognition by a carbazole-based neutral tripodal receptor in a competitive environment
2012
Anion recognition studies have been carried out on a series of neutral synthetic receptors in which carbazole-2-carboxamide has been used as building block. Different ligands which include one to three carbazole units in their structure have been prepared. Binding experiments have been performed under competitive conditions in DMSO and DMSO-water solutions. The tripodal receptor offered a better host-guest association due to the synergistic effect of a well arranged set of hydrogen bonds. A selective response towards the biologically important pyrophosphate anion has been achieved. This selectivity is enhanced when studies are carried out with an increasing water content, which gets as high…
Neutral nido-heteroboranes with non ionisable hydrogen as arenes in coordination
2003
Designed ligands have been synthesised to produce the first arene-like metallacarborane. For arene-like coordination the number of electronegative elements on the coordinating site must be kept to a minimum. Choosing ligands with bulky substituents on the heteroatom allows easy rearrangement and arene-like coordination. This is more hampered the higher the number of hetereoatoms to be re-located.
Exploring the 2,2′-Diamino-5,5′-bipyrimidine Hydrogen-Bonding Motif: A Modular Approach to Alkoxy-Functionalized Hydrogen-Bonded Networks
1998
The programmed self-association of 2,2’-diamino-4,4’-dialkoxy-5,5’-bipyrimidines allows for the de novo construction of alkoxy-functionalized H-bonded ribbons and sheets as evidenced by X-ray crystallographic analysis. The data provide insight into the interplay of the different structural and interactional features of the molecular components to the generation of the supramolecular assembly. Hydrophobicity of the didodecyl side chains of 4c leads to the dominance of the H-bonding factor, resulting in the formation of a fully interconnected array. These results define the utility of the of 2,2’-diamino-4,4’-dialkoxy-5,5’-bipyrimidines as a potential scaffold for the attachment of electro- o…
Stabilized Ru[(H2O)(6)](3+) in Confined Spaces (MOFs and Zeolites) Catalyzes the lmination of Primary Alcohols under Atmospheric Conditions with Wide…
2018
[EN] Imines are ubiquitous intermediates in organic synthesis, and the metal-mediated imination of alcohols is one of the most direct and simple methods for their synthesis. However, reported protocols lack compatibility with many other functional groups since basic supports/media, pure oxygen atmospheres, and/or released hydrogen gas are required during reaction. Here we show that, in contrast to previous metal-catalyzed methods, hexa-aqueous Ru(III) catalyzes the imination of primary alcohols with very wide functional group tolerance, at slightly acid pH and under low oxygen atmospheres. The inorganic metal complex can be supported and stabilized, integrally, within either faujasite-type …