Takeuchi K, Kohn T J, Mais D E, True T A, Wyss V L, Jakubowski J A
Lilly Research Laboratories, Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, Indiana 46285, USA.
Bioorg Med Chem Lett. 1998 Aug 4;8(15):1943-8. doi: 10.1016/s0960-894x(98)00353-9.
Synthesis and initial in vitro evaluation of a novel series of phenyl oxazole derivatives are described. An SAR study of the novel dual-acting TRA/TSI agent has revealed that the lipophilicity of the oxazole amide substituents greatly influences the TRA activity but not the TSI. The chain length of the alkenoic acid side chain affects both TRA and TSI. The optimal chain length for the combined activities was found to be n = 4 (heptenoic acid).
描述了一系列新型苯基恶唑衍生物的合成及其初步体外评估。对新型双作用促甲状腺素受体激动剂/促甲状腺素抑制性免疫球蛋白（TRA/TSI）药物的构效关系（SAR）研究表明，恶唑酰胺取代基的亲脂性对TRA活性有很大影响，但对TSI无影响。链烯酸侧链的长度对TRA和TSI均有影响。发现联合活性的最佳链长度为n = 4（庚烯酸）。
