Synthesis and biological evaluation of 2,3-diazabicyclo[2.2.1]heptane derivatives as prostaglandin endoperoxide analogs
β Scribed by Sheung-Tsam Kam; Robert N. Hanson; Philip S. Portoghese
- Publisher
- John Wiley and Sons
- Year
- 1980
- Tongue
- English
- Weight
- 505 KB
- Volume
- 69
- Category
- Article
- ISSN
- 0022-3549
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β¦ Synopsis
Three prostaglandin endoperoxide analogs that possess the 2,3-diazabicyclo[2.2.1]heptane skeleton were synthesized and evaluated for activity in human platelets and in the rat fundus. All three compounds were inactive in inhibiting or stimulating platelet aggregation. One compound possessed weak contracting activity on the rat fundus.
π SIMILAR VOLUMES
## Abstract Thirtyβseven (most of them novel) chiral derivatives of (1__S__,4__S__)β2,5βdiazabicyclo[2.2.1]heptane (**2**β**36**, **38**, **39**) were prepared from (__S__)β__trans__β4βhydroxyproline. A selection of these chiral ligands were examined as potential ligands in the preparation of catal
Since the discovery that the prostaglandin endoperoxides PGG2 and PGH2 are convertedenzymically to the highly unstable but biologically potent substance thromboxane A2 l-3 by a relatively straightforward mechanism, it has been clear that various synthetic analogs of the PG endoperoxides would be of