4289-36-5Relevant articles and documents
NCN trianionic pincer ligand precursors: Synthesis of bimetallic, chelating diamide, and pincer group IV complexes
Sarkar, Soumya,McGowan, Kevin P.,Culver, Jeffrey A.,Carlson, Adam R.,Koller, Juergen,Peloquin, Andrew J.,Veige, Melanie K.,Abboud, Khalil A.,Veige, Adam S.
experimental part, p. 5143 - 5156 (2010/08/21)
This report details the synthesis of new NCN trianionic pincer ligand precursors and metalation reactions to form group (IV) complexes. N,N-[1,3-phenylenebis(methylene)]bis-2,6-diisopropylaniline [2,6- iPrNCN]H3 (8) was converted to
Synthesis and structure-activity relationships of azamacrocyclic C-X-C chemokine receptor 4 antagonists: Analogues containing a single azamacrocyclic ring are potent inhibitors of T-cell tropic (X4) HIV-1 replication
Bridger, Gary J.,Skerlj, Renato T.,Hernandez-Abad, Pedro E.,Bogucki, David E.,Wang, Zhongren,Zhou, Yuanxi,Nan, Susan,Boehringer, Eva M.,Wilson, Trevor,Crawford, Jason,Metz, Markus,Hatse, Sigrid,Princen, Katrien,De Clercq, Erik,Schols, Dominique
supporting information; experimental part, p. 1250 - 1260 (2010/08/07)
Bis-tetraazamacrocycles such as the bicyclam AMD3100 (1) are a class of potent and selective anti-HIV-1 agents that inhibit virus replication by binding to the chemokine receptor CXCR4, the coreceptor for entry of X4 viruses. By sequential replacement and/or deletion of the amino groups within the azamacrocyclic ring systems, we have determined the minimum structural features required for potent antiviral activity in this class of compounds. All eight amino groups are not required for activity, the critical amino groups on a per ring basis are nonidentical, and the overall charge at physiological pHcan be reduced without compromising potency. This approach led to the identification of several single ring azamacrocyclic analogues such as AMD3465 (3d), 36, and 40, which exhibit EC50's against the cytopathic effects of HIV-1 of 9.0, 1.0, and 4.0 nM, respectively, antiviral potencies that are comparable to 1 (EC50 against HIV-1 of 4.0 nM). More importantly, however, the key structural elements of 1 required for antiviral activitymay facilitate the design of nonmacrocyclic CXCR4 antagonists suitable for HIV treatment via oral administration. 2009 American Chemical Society.
INHIBITORS OF MACROPHAGE MIGRATION INHIBITORY FACTOR
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Page/Page column 53, (2010/12/29)
The invention provides the use of isothiocyanate and isoselenocyanate compounds for treating diseases and conditions mediated by MIF.
Bisphosphonate sequestering agents. Synthesis and preliminary evaluation for in vitro and in vivo uranium(VI) chelation
Sawicki, Marcin,Lecercle, Delphine,Grillon, Gerard,Le Gall, Beatrice,Serandour, Anne-Laure,Poncy, Jean-Luc,Bailly, Theodorine,Burgada, Ramon,Lecouvey, Marc,Challeix, Vincent,Leydier, Antoine,Pellet-Rostaing, Stephane,Ansoborlo, Eric,Taran, Frederic
experimental part, p. 2768 - 2777 (2009/04/06)
A library of bisphosphonate-based ligands was prepared using solution-phase parallel synthesis and tested for its uranium-binding properties. With the help of a screening method, based on a chromophoric complex displacement procedure, 23 dipodal and tripodal chelates bearing bisphosphonate chelating functions were found to display very high affinity for the uranyl ion and were selected for evaluation of their in vivo uranyl-removal efficacy. Among them, 11 ligands induced a huge modification of the uranyl biodistribution by deviating the metal from kidney and bones to liver. Among the other ligands, the most potent was the dipodal bisphosphonate 3C which reduced the retention of uranyl and increased its excretion by around 10% of the injected metal.
Exploiting protein fluctuations at the active-site Gorge of human cholinesterases: Further optimization of the design strategy to develop extremely potent inhibitors
Butini, Stefania,Campiani, Giuseppe,Borriello, Marianna,Gemma, Sandra,Panico, Alessandro,Persico, Marco,Catalanotti, Bruno,Ros, Sindu,Brindisi, Margherita,Agnusdei, Marianna,Fiorini, Isabella,Nacci, Vito,Novellino, Ettore,Belinskaya, Tatyana,Saxena, Ashima,Fattorusso, Caterina
experimental part, p. 3154 - 3170 (2009/04/06)
Protein conformational fluctuations are critical for biological functions, although the relationship between protein motion and function has yet to be fully explored. By a thorough bioinformatics analysis of cholinesterases (ChEs), we identified specific hot spots, responsible for protein fluctuations and functions, and those active-site residues that play a role in modulating the cooperative network among the key substructures. This drew the optimization of our design strategy to discover potent and reversible inhibitors of human acetylcholinesterase and butyrylcholinesterase (hAChE and hBuChE) that selectively interact with specific protein substructures. Accordingly, two tricyclic moieties differently spaced by functionalized linkers were investigated as molecular yardsticks to probe the finest interactions with specific hot spots in the hChE gorge. A number of SAR trends were identified, and the multisite inhibitors 3a and 3d were found to be the most potent inhibitors of hBuChE and hAChE known to date.
Antiviral compounds
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, (2008/06/13)
The present invention is drawn to novel antiviral compounds, pharmaceutical compositions and their use. More specifically this invention is drawn to derivatives of monocyclic polyamines which have activity in standard tests against HIV-infected cells as w
Sulfonamides of phenylalkylamines or phenoxyalkylamines processes for their preparation and medicaments containing these compounds
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, (2008/06/13)
Compounds of the formula I STR1 in which R1 signifies an aryl, aralkyl or an aralkenyl group, the aryl radical of which can, in each case, be substituted one or more times by halogen, cyano, alkyl, trifluoromethyl, alkoxy, alkylthio, trifluoromethoxy, hydroxyl or carboxyl, m a whole number from 1 to 3, n a whole number from 1 to 5, R2 hydrogen, an alkyl, aralkyl or acyl group, Q a bond or an oxygen atom, R3 hydrogen or a lower alkyl radical which is possibly terminally substituted by carboxyl or by a hydroxyl group and R4 hydrogen, a lower alkyl group with 1-4 C-atoms, which is possibly terminally substituted by carboxyl or hydroxyl, a possibly substituted phenyl, heteroaryl, cycloalkyl or acyl group or a group STR2 in which R5 represents a straight-chained or branched alkyl chain with 1-4 C-atoms which is possibly terminally substituted by carboxyl, alkoxycarbonyl, aminocarbonyl, hydroxyl, mercapto, alkylthio or imidazolyl and Y a carboxyl, an alkoxycarbonyl, aminocarbonyl or cyano, formyl, hydroxymethyl, aminomethyl or ortho ester group, whereby R3 and R4 can also be component of a 5- or 6-membered saturated or unsaturated possibly substituted heterocycle with 1-4 heteroatoms which can be annellated with further ring compounds via one or more bonds, as well as their salts, esters and amides, processes for their preparation and medicaments with thromboxane-antagonistic action which contain these compounds.
Inclusion Compounds of Organic Onium Salts, IV. Organyl Ammonium Hosts as Versatile Clathrate Formers
Loehr, Hans-Gerd,Josel, Hans-Peter,Engel, Aloys,Voegtle, Fritz,Schuh, Willy,Puff, Heinrich
, p. 1487 - 1496 (2007/10/02)
The organyl-oligo-ammonium compounds 1 - 25 and their clathrates with a variety of low molecular weight neutral compounds, especially solvent molecules, are prepared.The inclusion capacity of the new clathrands can be explained by interstices in the host lattice.The conformational flexibility of the voluminous onium branches is responsible for the great number of clathrates; their stability depends on the ion lattice.The X-ray analysis of the ethanol clathrate of the onium host 8 shows that one ethanol molecule is surrounded by the host molecules in a cage-type manner.The great variety of the inclusions obtained up to now demonstrates that the oligo onium host compounds have to be considered as the most universal clathrands of organic chemistry.Hints are given for the syntheses of new onium clathrates.
