Synthesis of a chemically and metabolically stable and biologically potent PGD2-analogue

✍ Scribed by B. Buchmann; W. Skuballa; H. Vorbrüggen

• Publisher: Elsevier Science
• Year: 1990
• Tongue: French
• Weight: 287 KB
• Volume: 31
• Category: Article
• ISSN: 0040-4039
• DOI: 10.1016/s0040-4039(00)97413-6

✦ Synopsis

The mtabolic labile a-chain of the FGD -analogue 2 (ZK 110841) can be stabiied by introduction of an @oxygen-atom resulting in 3 (Z&K l&82), whicrhss a much higher and longer lasting bioh@cal activity. on oml application in rats. The synthetic methodology for the synthesis of 3-oxa-&A 1 -prostagl~ will be discussed.

Erostaglsndin & (FGD2) 1. is the major cyclooxygenase product in the central nervous system') and can induce sleep in the brain2). PGD2, which is also synthesized by platelets, is furthermore a very strong vasodilator and inhibitor of blond-platelet aggmgation3) and exerts these effects through a distinct receptor different from the prostacyclin (EGIi) and prostaglandin Et receptors.