Hidekado Tokumoto

Molecular design of novel PGI2 agonists without PG skeleton. III

Abstract Syntheses of novel prostaglandin (PG) mimetics without PG skeleton are described, and the structure-activity relationships are discussed. Highly potent compounds could be obtained when the PG analog 3 was modified by removing and reconstructing the cyclopentane ring, and changing the allylic alcohol in the natural PGs.

Pharmacological evaluation of combined PGI2 agonists/thromboxane synthase inhibitors. I

Abstract By incorporation of a pyridine moiety into compounds shown to be PGI 2 agonists, we have synthesized a series of compounds which also show potent thromboxane synthase inhibitory activity. Agents 9 and 14 with the 3-substituted pyridine moiety show a combined properties of PGI 2 agonist and TXA 2 synthase inhibitor.