Search results for "Amide"
showing 10 items of 3119 documents
N-Isopropylacrylamide andN-Isopropylmethacryl-amide: Cloud Points of Mixtures and Copolymers
2001
The cloud point curve of aqueous solutions of poly(N-isopropylacrylamide), poly(N-isopropylmethacrylamide) and their statistical copolymers were determined turbidimetrically. All the Systems demix upon heating at the cloud point temperature and mix reversibly upon cooling. The cloud points are independent of the total concentration of the solutions (dilute range) and of the sample thickness. Mixtures of the homopolymers poly(N-isopropylacrylamide) and poly(N-isopropylmethacrylamide) in water (ternary systems) exhibit two cloud points, which are nearly the same as the cloud points of the two binary systems homopolymer/water. A quantitative correlation was found between the cloud point temper…
Characterization of a Novel Type of Serine/Threonine Kinase That Specifically Phosphorylates the Human Goodpasture Antigen
1999
Goodpasture disease is an autoimmune disorder that occurs naturally only in humans. Also exclusive to humans is the phosphorylation process that targets the unique N-terminal region of the Goodpasture antigen. Here we report the molecular cloning of GPBP (Goodpasture antigen-binding protein), a previously unknown 624-residue polypeptide. Although the predicted sequence does not meet the conventional structural requirements for a protein kinase, its recombinant counterpart specifically binds to and phosphorylates the exclusive N-terminal region of the human Goodpasture antigen in vitro. This novel kinase is widely expressed in human tissues but shows preferential expression in the histologic…
2-Cinnamamido, 2-(3-phenylpropiolamido), and 2-(3-phenylpropanamido)benzamides: synthesis, antiproliferative activity, and mechanism of action
2013
Abstract Several new benzamides 4a–q were synthesized by stirring in pyridine the acid chlorides 3a–q with the appropriate anthranilamide derivatives 2a–g. Some of the synthesized compounds were evaluated for their in vitro antiproliferative activity against a panel of 5 human cell lines (K562 human chronic myelogenous leukemia cells, MCF-7 breast cancer cells, HTC-116 and HT26 colon cancer cells and NCI H460 non-small cell lung cancer cells).
Colorimetric sensing of anions by a neutral biphenyl based amide receptor
2007
A new colorimetric sensor for fluoride is described. Compound 1 shows an open structure and its behaviour is compared with that of two related closed compounds 2 and 3. In all cases, the red colour developed in the presence of fluoride can be related to deprotonation processes, however ligand 1 gives rise to a faster colour change than 2 or 3 because of its higher flexibility. Other halides as well as carboxylates have been studied and the stoichiometry and complexation constants for the corresponding ligands have been determined. Costero Nieto, Ana Maria, Ana.Costero@uv.es ; Peransi Llopis, Sergio Manuel, Sergio.Peransi@uv.es
Structure‐Activity Relationships of Benzamides and Isoindolines Designed as SARS‐CoV Protease Inhibitors Effective against SARS‐CoV‐2
2020
Abstract Inhibition of coronavirus (CoV)‐encoded papain‐like cysteine proteases (PLpro) represents an attractive strategy to treat infections by these important human pathogens. Herein we report on structure‐activity relationships (SAR) of the noncovalent active‐site directed inhibitor (R)‐5‐amino‐2‐methyl‐N‐(1‐(naphthalen‐1‐yl)ethyl) benzamide (2 b), which is known to bind into the S3 and S4 pockets of the SARS‐CoV PLpro. Moreover, we report the discovery of isoindolines as a new class of potent PLpro inhibitors. The studies also provide a deeper understanding of the binding modes of this inhibitor class. Importantly, the inhibitors were also confirmed to inhibit SARS‐CoV‐2 replication in …
Oligo(phenylenevinylene)s with reactive side chains: amine- and amide-bound alkoxysilanes
2002
Strongly luminescent oligo(phenylenevinylene) chromophores with monodisperse chain lengths are connected via short spacers containing a secondary amine or amide with di- and tri-ethoxysilane groups. The alkoxysilanes can be hydrolysed and condensed to cyclic and linear oligomers with high film forming capability and are also interesting functional units for hybrid materials for electro-optical applications. The luminescence properties in the solid state are influenced by hydrogen bonding of the amides resulting in strong hypsochromic shifts. The synthesis of the title compounds, their oligomerisation and the electronic spectra in the solution and solid state are presented.
Interaction ofEscherichia colihemolysin with biological membranes
2001
Escherichia coli hemolysin (HlyA) is a membrane-permeabilizing protein belonging to the family of RTX-toxins. Lytic activity depends on binding of Ca2(+) to the C-terminus of the molecule. The N-terminus of HlyA harbors hydrophobic sequences that are believed to constitute the membrane-inserting domain. In this study, 13 HlyA cysteine-replacement mutants were constructed and labeled with the polarity-sensitive fluorescent probe 6-bromoacetyl-2-dimethylaminonaphthalene (badan). The fluorescence emission of the label was examined in soluble and membrane-bound toxin. Binding effected a major blue shift in the emission of six residues within the N-terminal hydrophobic domain, indicating inserti…
Strong Cooperativity and Loose Geometry between CUB Domains Are the Basis for Procollagen C-Proteinase Enhancer Activity
2009
Procollagen C-proteinase enhancers (PCPE-1 and -2) specifically activate bone morphogenetic protein-1 (BMP-1) and other members of the tolloid proteinase family during C-terminal processing of fibrillar collagen precursors. PCPEs consist of two CUB domains (CUB1 and CUB2) and one NTR domain separated by one short and one long linker. It was previously shown that PCPEs can strongly interact with procollagen molecules, but the exact mechanism by which they enhance BMP-1 activity remains largely unknown. Here, we used a series of deletion mutants of PCPE-1 and two chimeric constructs with repetitions of the same CUB domain to study the role of each domain and linker. Out of all the forms teste…
An Na8 Cluster in the Structure of a Novel oxamato-bridged Na'Cu'' three-Dimensional Coordination Polymer
1999
[EN] The new heterometallic sodium(I)¿copper(II) compound Na4Cu2 (2) · 10.5 H2O (3), where H8[2] stands for N,N',N'',N'''-methanetetrayltetrakismethylenetetrakis(oxamic acid), has been synthesized and its crystal structure determined by single-crystal X-ray diffraction. The structure of 3 consists of cationic [Cu2(¿4:¿4-2)]4- dinuclear units, coordinated sodium cations, and water molecules. In the crystal, the dinuclear copper entities are joined through discrete aggregates of eight sodium atoms linked by oxamato and water bridges, leading to a three-dimensional polymeric network.
Zinc(II) complexes of amide- and urea-substituted 8-hydroxyquinolines
2002
Abstract A series of amide- and urea-substituted 8-hydroxyquinoline ligands 1–6-H are used for the formation of zinc(II) complexes. Hereby in general 2:1 complexes are obtained and the X-ray structure of [(3)2Zn] reveals the presence of a coordination polymer in the solid state. Only the derivatives of 7-amino-8-hydroxyquinoline 4-H and 5-H form trinuclear hexa-helical 6:3 complexes which exhibit interesting structural and NMR and fluorescence spectroscopic properties.