SYNTHESIS AND BIOLOGICAL ACTIVITIES OF BIOISOSTERIC O-CARBA-ANALOGUES OF PLATELET ACTIVATING FACTOR (PAF)

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説明

Four types of O-carba-analogues of C16-PAF were synthesized : d1-2-acetoxyeicosylphosphoryl choline (1), dl-3-hexadecyloxy-2-(2-oxopropyl) propylphosphoryl choline (2), d1-and (S)-(-)-3-acetoxy-4-hexa-decyloxybutylphosphonyl choline (3), and d1-2-acetoxy-3-hexadecyloxypropyl (3-trimethylammonio) propylphosphonate (4). Both in hypotension and in platelet aggregation, (S)-(-)-3 was one third as potent as synthetic C16-PAF, whereas 1, 2 and 4 were 100-3, 000 times less potent.

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