Syntheses and platelet aggregation inhibitory and antithrombotic properties of (2-(( omega -Aminoalkoxy) phenyl) ethyl) benzenes

A series of (2-(( omega -aminoalkoxy)phenyl)ethyl) benzene derivatives were synthesized and evaluated for their ability to inhibit collagen-induced platelet aggregation in vitro and to protect experimental thrombosis in mice. The results showed that the compounds were in vitro inhibitors of collagen...

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Bibliographic Details
Published in:Journal of medicinal chemistry 1990-01, Vol.33 (6), p.1818-1823
Main Authors: Kikumoto, R, Hara, H, Ninomiya, K, Osakabe, M, Sugano, M, Fukami, H, Tamao, Y
Format: Article
Language:English
Subjects:
benzene
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Summary:A series of (2-(( omega -aminoalkoxy)phenyl)ethyl) benzene derivatives were synthesized and evaluated for their ability to inhibit collagen-induced platelet aggregation in vitro and to protect experimental thrombosis in mice. The results showed that the compounds were in vitro inhibitors of collagen-induced platelet aggregation. Most of them were also effective in the mouse antithrombotic assay. The compounds were found to be potent antagonists to S sub(2) serotonergic receptors, and good correlation (r = 0.85) between their S sub(2) serotonergic receptor antagonism and their potency as platelet, antiaggregatory drugs was observed. Among the compounds studied mono(2-(dimethylamino)-1-((2-(2-(3-methoxyphenyl)ethyl)phenoxy)met hyl)ethyl) succinate hydrochloride (12b, MCI-9042) was selected for further pharmacological and toxicological evaluation.
ISSN:0022-2623