133226-75-2Relevant 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).
