Synthesis and platelet aggregation inhibiting activity of prostaglandin D analogs
- 1 June 1983
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 26 (6), 790-799
- https://doi.org/10.1021/jm00360a003
Abstract
Several prostaglandin D (PGD) analogs were synthesized, incorporating the following variations: varying degrees of side-chain unsaturation, C-9 hydroxy removed or in the unnatural 9.beta. configuration, metabolically stabilized analog (e.g., 15-methyl, 16,16-dimethyl, 17-phenyl, etc) and .DELTA.12 isomers resulting from decomposition of PGD2. With regard to their ability to inhibit ADP induced human platelet aggregation: PGD3 .gtoreq. PGD2 > PGD1 > 13,14-dihydro-PGD1; the 9.beta.- and 9-deoxy-PGD2 analog are more potent than PGD2; metabolically stabilized analogs with bulky substituents at or near C-15 have substantially reduced antiaggregatory activity relative to PGD2; and the .DELTA.12 isomers of PGD2 are much less active than PGD2.This publication has 9 references indexed in Scilit:
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