108664-90-0Relevant academic research and scientific papers
Extended fluorescent uridine analogues: synthesis, photophysical properties and selective interaction with BSA protein
Ardhapure, Ajaykumar V.,Bag, Subhendu Sekhar,Bhilare, Shatrughn,Gayakhe, Vijay,Gunturu, Krishna Chaitanya,Kapdi, Anant R.,Sanghvi, Yogesh S.
, p. 14744 - 14754 (2020)
The improvement in fluorescence properties of 2′-deoxyuridine was brought about by the introduction of (hetero)aromatic moieties at the C-5 position of uridine directly orviaalkenyl/phenyl/styryl linkers to create a library of biologically useful fluorescent nucleosides. The synthesis of these extended nucleoside analogues was carried out using Suzuki-Miyaura and Heck alkenylation reactions. A comparison of their photophysical properties allowed the identification of nucleosides1gand1hthat exhibit the highest quantum yields in an aqueous solution. Studies on the binding interaction of the most promising fluorescent analogues,1gand1h, with serum albumin proteins showed excellent selectivity towards BSA protein over α-amylase. Docking studies were also performed to predict the specific binding site of the nucleosides to BSA.
Simplifying the conductance profiles of molecular junctions: The use of the trimethylsilylethynyl moiety as a molecule-gold contact
Marques-Gonzalez, Santiago,Yufit, Dmitry S.,Howard, Judith A.K.,Martin, Santiago,Osorio, Henrry M.,Garcia-Suarez, Victor M.,Nichols, Richard J.,Higgins, Simon J.,Cea, Pilar,Low, Paul J.
, p. 338 - 341 (2013/03/14)
Conductance across a metal|molecule|metal junction is strongly influenced by the molecule-substrate contacts, and for a given molecular structure, multiple conductance values are frequently observed and ascribed to distinct binding modes of the contact at each of the molecular termini. Conjugated molecules containing a trimethylsilylethynyl terminus, -C≡CSiMe 3 give exclusively a single conductance value in I(s) measurements on gold substrates, the value of which is similar to that observed for the same molecular backbone with thiol and amine based contacting groups when bound to under-coordinated surface sites.
One-point binding ligands for asymmetric gold catalysis: Phosphoramidites with a TADDOL-related but acyclic backbone
Teller, Henrik,Corbet, Matthieu,Mantilli, Luca,Gopakumar, Gopinadhanpillai,Goddard, Richard,Thiel, Walter,Fuerstner, Alois
supporting information, p. 15331 - 15342 (2012/11/07)
Readily available phosphoramidites incorporating TADDOL-related diols with an acyclic backbone turned out to be excellent ligands for asymmetric gold catalysis, allowing a number of mechanistically different transformations to be performed with good to outstanding enantioselectivities. This includes [2 + 2] and [4 + 2] cycloadditions of ene-allenes, cycloisomerizations of enynes, hydroarylation reactions with formation of indolines, as well as intramolecular hydroaminations and hydroalkoxylations of allenes. Their preparative relevance is underscored by an application to an efficient synthesis of the antidepressive drug candidate (-)-GSK 1360707. The distinctive design element of the new ligands is their acyclic dimethyl ether backbone in lieu of the (isopropylidene) acetal moiety characteristic for traditional TADDOLs. Crystallographic data in combination with computational studies allow the efficiency of the gold complexes endowed with such one-point binding ligands to be rationalized.
Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds
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, (2008/06/13)
The present invention relates to alkyne compounds of general formula I wherein the groups and residues A, B, W, X, Y, Z, R1 and R2 have the meanings given in claim 1. The invention further relates to pharmaceutical compositions containing at least one alkyne according to the invention. In view of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.
Linear Free Energy Relationship Studies of 5-Substituted 2,4-Dioxopyrimidine Nucleosides
Chang, George,Mertes, Mathias P.
, p. 3625 - 3631 (2007/10/02)
The development of a direct and efficient palladium(0)-catalyzed biaryl coupling reaction permitted the synthesis of a series of N1-substituted 5-aryl-2,4-dioxopyrimidines.The physical and spectral properties of these compounds were determined and correlated by various linear free energy relationships.The relationships between the physical and spectral data with Hammett ? constants proved useful in analyzing the electron distribution of the heterocycle.Although a significant degree of orbital overlap and interaction between the substituents and the pyrimidine ring was observed, it is doubtful that the interactions are comparable to those of a benzene ring system.
