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Structure-activity studies on antidepressant 2,2-diarylethylamines.

Abstract：

:A series of 2,2-diarylethylamine derivatives has been examined for potential antidepressant activity in the tetrabenazine (TBZ) test. Diethanolamine 4 (McN-4187) was one of the more potent compounds despite its polar alcohol functionalities [ED50 values of 15 mg/kg (exploratory activity) and 1.5 mg/kg (ptosis)]. Structure-activity relationships are described. Minor structural modifications of 4 were sufficient to strongly attenuate activity. For example, changing one phenyl group to a 2-thienyl, cyclohexyl, or 3,4-dimethoxyphenyl group greatly reduced activity. Replacing both phenyl groups by 4-chlorophenyl groups also dissipated activity. The bisethanol functionality was not essential for activity (q.v. 17-19 in Table I). Although 17-19 compared well with 4 in the TBZ assay, only 19 (like 4) showed a satisfactory profile in the maximal electroshock seizure threshold test.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Maryanoff BE,Nortey SO,Gardocki JF

doi

10.1021/jm00374a022

subject

Has Abstract

pub_date

1984-08-01 00:00:00

pages

1067-71

issue

8

eissn

0022-2623

issn

1520-4804

journal_volume

27

pub_type

杂志文章

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