Syntheses and platelet aggregation inhibitory and antithrombotic properties of [2-[(omega-aminoalkoxy)phenyl]ethyl]benzenes.

Abstract

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 S2 serotonergic receptor, and good correlation (r = 0.85) between their S2 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]methyl]ethyl] succinate hydrochloride (12b, MCI-9042) was selected for further pharmacological and toxicological evaluation.

• Authors: R Kikumoto, H Hara, K Ninomiya, M Osakabe, M Sugano, H Fukami, Y Tamao
• Journal: Journal of medicinal chemistry (J Med Chem) Vol. 33 Issue 6 Pg. 1818-23 (Jun 1990) ISSN: 0022-2623 [Print] United States
• PMID: 2342076 (Publication Type: Journal Article)

Chemical References

• Fibrinolytic Agents
• Platelet Aggregation Inhibitors
• Serotonin Antagonists
• Succinates
• sarpogrelate
• Collagen

Topics

• Animals
• Collagen
• Fibrinolytic Agents (chemical synthesis, pharmacology)
• Mice
• Platelet Aggregation Inhibitors (chemical synthesis, pharmacology)
• Rabbits
• Serotonin Antagonists
• Succinates (chemical synthesis, pharmacology)