85311-31-5Relevant academic research and scientific papers
PAF-antagonists with phospholipid structure. Part 2: Phospholipids with heteroarene head groups and variation of the P-N-distance; synthesis, characterization and structure-activity relationships
Kertscher,Ostermann
, p. 708 - 711 (2007/10/02)
A series of 27 PAF-analogues with heteroarene head groups and variation of the P-N-distance on the C-3-position of the backbone were synthesized, and the PAF-antagonistic activity on human blood platelets in vitro was evaluated. Investigation of structure-activity relationships revealed that PAF-antagonistic activity is strongly influenced by the 4-(Dimethylamino)-pyridine as polar head base and the distance between phosphate group and onium center. Maximal activity was observed with a chain length of 3 or 4 methylene groups. Among the compounds tested, 1-O-Hexadecyl-2-n-propylpropan-1,3-diol-3-phosphoric acid-4'-[4-(dimethylamino)pyridinium]butylester was the most effective inhibitor in the in vitro assay (K(B) = 0,3 μmol/l).
Synthesis and biological activity of some lysing and fusogenically active phosphocholine derivatives
Nuhn,Kertscher,Dobner,Braune,Kluge
, p. 706 - 708 (2007/10/02)
2-Hexadecylglycerophosphocholine (1) and its 1-O-methyl, 1-O-ethyl and 1-O-benzyl (4) derivatives as well as some n-alkanol phosphocholines were synthetized and tested for haemolytic activity. Most potent (LD50 approximately equal to 5.10(-6) mol/l) were 1 and the hexadecanol and octadecanol phosphocholines (7 and 8). 1, 4 and 7 were tested for fusogenic activity against vegetable protoplasts. When used at sublytic concentrations (0.01 - 0.05 mmol), these compounds were as efficient as polyethylene glycol.
