Anticoagulant activity of amino acid modified polystyrene resins: influence of the carboxylic acid function

Biomaterials ◽  
1983 ◽  
Vol 4 (2) ◽  
pp. 101-104 ◽  
Author(s):  
C. Fougnot ◽  
M.P. Dupillier ◽  
M. Jozefowicz
Tetrahedron ◽  
1987 ◽  
Vol 43 (8) ◽  
pp. 1857-1861 ◽  
Author(s):  
Geoffrey N. Austin ◽  
Peter D. Baird ◽  
Hak-Fun Chow ◽  
L.E. Fellows ◽  
G.W.J. Fleet ◽  
...  

1956 ◽  
Vol 34 (10) ◽  
pp. 1444-1446 ◽  
Author(s):  
Gordon A. Grant ◽  
Carl Von Seemann ◽  
Stanley O. Winthrop

A number of β-dialkylaminoethyl esters of 2,5-disubstituted pyrimidine-4-carboxylic acids have been synthesized and characterized as their hydrochlorides and in some cases as their methobromide and methiodide salts. Mucochloric acid has been condensed with S-methylisothiouronium sulphate to give 2-methylthio-5-chloropyrimidine-4-carboxylic acid, and the corresponding 5-bromo- acid has been converted to the 5-amino-acid.


2013 ◽  
Vol 91 (1) ◽  
pp. 66-81 ◽  
Author(s):  
Pierre L. Beaulieu ◽  
René Coulombe ◽  
James Gillard ◽  
Christian Brochu ◽  
Jianmin Duan ◽  
...  

Acylsulfonamide and acylsulfamide as surrogates for the carboxylic acid function of N-acetamide-indole-6-carboxylic acids were evaluated as allosteric inhibitors of hepatitis C virus (HCV) NS5B polymerase. Several analogs displayed excellent antiviral potency against both 1a and 1b HCV genotypes in cell-based subgenomic replicon assays. Structure–activity relationships (SAR) are discussed in the context of the crystal structure of an inhibitor − NS5B polymerase complex. Absorption, distribution, metabolism, and excretion pharmacokinetic (ADME-PK) properties of this class of inhibitors are also described.


2001 ◽  
Vol 125 (4) ◽  
pp. 1620-1632 ◽  
Author(s):  
Céline Delétage-Grandon ◽  
Jean-François Chollet ◽  
Mireille Faucher ◽  
Francoise Rocher ◽  
Ewald Komor ◽  
...  
Keyword(s):  

1983 ◽  
Vol 210 (3) ◽  
pp. 789-794 ◽  
Author(s):  
A Weber ◽  
E W Westhead ◽  
H Winkler

1. The influence of various substances on the uptake of [3H]ATP and [14C]-noradrenaline into isolated bovine chromaffin granules was investigated. The carrier-mediated [3H]ATP uptake is specifically inhibited by SO42-, PO43- and phosphoenolpyruvate. Compounds with carboxylic acid or sulphonic acid groups had no significant inhibitory effects on either uptake. 2. 35SO42-, 32PO43- and phosphoenol[14C]pyruvate are taken up into chromaffin granules by a temperature-dependent process that is inhibited by atractyloside, uncouplers of oxidative phosphorylation and lipid-permeant anions. The apparent Km of 35SO42- uptake is 0.4 mM. 3. These results indicate that the nucleotide carrier in chromaffin granules has a broad specificity, transporting compounds with two strong negative charges. 4. Amino acid probes influence the uptake of ATP and catecholamines differently. Pyridoxal phosphate inhibits both uptake processes, 4,4′-di-isothiocyanostilbene-2,2′-disulphonic acid preferentially blocks ATP uptake, whereas phenylglyoxal blocks only ATP transport. It is suggested that the nucleotide carrier possesses arginine residues in a functionally important position. 5. The significance of these results obtained on isolated granules for the function of chromaffin granules within the cell is discussed.


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