Affordable Access

Thromboxane A2 receptor antagonists. I. Synthesis and pharmacological activity of 7-oxabicyclo-[2.2.1]heptane derivatives with the benzenesulfonylamino group.

Authors
Type
Published Article
Journal
Chemical & pharmaceutical bulletin
Publication Date
Volume
37
Issue
2
Pages
327–335
Identifiers
PMID: 2525965
Source
Medline
License
Unknown

Abstract

Four stereoisomers of 7-oxabicyclo[2.2.1]heptane derivatives with the benzenesulfonylamino group, 11, 14, 23 and 33, were synthesized and their sodium salts were examined in vitro for inhibitory activity against aggregation of rabbit platelet-rich plasma and of rat washed platelets. The trans-isomer 23 exhibited high potency but showed a partial agonistic effect. Compound 11 did not show a partial agonistic effect, though it was a less active inhibitor. The following trans compounds were synthesized and their IC50 values were measured: homologated trans-isomers with one methylene chain (47 and 53), an olefin derivative (58), and optically active derivatives [-)-11 and (+)-23).

Statistics

Seen <100 times