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Abstract
Novelty: Aryl, amide, imide and carbamate derivatives of pyridine are disclosed as antagonists of PAF. They may be used to treat asthma, endotoxic shock, transplant rejection, thrombosis, stroke and cancer.
Biology: In vitro PAF antagonism was assayed using blood from NZ rabbits and inhibition of aggregation was 0-97%. In vivo survival after PAF-induced lethality in mice was increased by 0-69% in two hours and survival out of fifteen from acute endotoxaemia was increased to 0-14 (control, endotoxin only = 0-6).
Chemistry: One hundred and forty-eight examples of syntheses of the compounds by standard techniques are provided. Characterization is by mp, ms and elemental analysis. A preferred compound is 2-[[acetyl[4-(tetradecyloxy)benzoyl]amino]methyl]-1-methylpyridinium iodide.