Synthesis and structure-activity relationships of oxamic acid and acetic acid derivatives related to L-thyronine

N Yokoyama, GN Walker, AJ Main…

文献索引：Yokoyama, Naokata; Walker, Gordon N.; Main, Alan J.; Stanton, James L.; Morrissey, Michael M.; et al. Journal of Medicinal Chemistry, 1995 , vol. 38, # 4 p. 695 - 707

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被引用次数: 87

摘要

Aryloxamic acids 7 and 23,(ary1amino) acetic acids 29, arylpropionic acids 33, arylthioacetic acids 37, and (ary1oxy) acetic acid 41 related to L-triiodothyronine (L-T3) were prepared and tested in vitro for binding to the rat liver nuclear L-T3 receptor and the rat membrane L- T3 receptor. The structure-activity relationships for these compounds are described, with 7f, 23a, 29c, 33a, 37b, and 41 showing excellent potency (IC60ps of 0.19, 0.16, 1.1, 0.11, 3.5, ...