Syntheses and Platelet Aggregation Inhibitory and Antithrombotic Properties of ethyl>benzenes

Article abstract of DOI:10.1021/jm00168a043

A series of <2-<(ω-aminoalkoxy)phenyl>ethyl>benzene derivatives were synthesized and evaluated for their ability to inhibit collagen-induced platelet aggregation in vitro and to protect experimantal 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.