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PubMed1991

[PAF-antagonists with a phospholipid structure. 1. Phospholipids with hetero-arene head groups: synthesis, characterization and determination of the action of structural elements].

A series of analogues of platelet-activating factor (PAF) with heteroarene head groups have been synthesized, and tested for biological activities on blood platelets in vitro. In comparison with PAF most of the structural modifications exerted weak proaggregatory effects. The 4-(dimethylamino)pyridinium compound did not activate platelets but inhibited selectively PAF-induced platelet responses. These results point to a crucial role of the distance between the phosphoryl group and polar head for expression of PAF-antagonistic properties. Structural features of PAF-antagonist have been investigated by two-dimensional proton NMR spectroscopy, and proposed a model with three-dimensional structure.

Blood Platelets↗
PubMed1991

[PAF-antagonists with phospholipid structure. 2. Phospholipids with heteroarene head groups and variations of the phosphorus-nitrogen distance; synthesis, characterization and structure-activity relationships].

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 (KB = 0.3 mumol/l).

Chromatography, Thin Layer↗
PubMed1991

[PAF-antagonists with phospholipid structure. 3. Phospholipids with heterocyclane head groups and variations of the phosphorus-nitrogen distance; synthesis, characterization and structure-activity relationship].

A series of 13 PAF-analogues with heterocyclane head groups and variation of the P-N-distance on the C-3-position of the backbone were synthesized. The proaggregatory and inhibitory potencies on rabbit and human blood platelets in vitro was evaluated. Investigations of structure-activity relationship revealed that the PAF-inhibitory potency is strongly influenced by the distance between phosphate and onium center and the structure of the heterocyclane. Derivatives with a P-N-distance of 4 or more methylene groups emerged effective inhibitors. The best activity was observed by chinuclidine- and N-methylpiperidine analogues with a chain length of 6 methylene groups (KB = 1.1 to 2.3 mumol/l).

Animals↗