首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and pharmacological evaluation of new 4-2-(7-heterocyclemethoxynaftalen-2-ylmethoxy)ethylbenzoic acids as LTD(4)-antagonists.
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Synthesis and pharmacological evaluation of new 4-2-(7-heterocyclemethoxynaftalen-2-ylmethoxy)ethylbenzoic acids as LTD(4)-antagonists.

机译:新型4-2-(7-杂环甲氧基萘基-2-基甲氧基)乙基苯甲酸作为LTD(4)-拮抗剂的合成及药理评价。

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摘要

A group of new 4-[2-(7-heterocyclemethoxynaftalen-2-ylmethoxy)ethyl]benzoic acids have been synthesized and pharmacologically evaluated as LTD(4)-antagonists. Thiazole derivatives, especially 4-[2-[7-(4-cyclobutylthiazole-2-ylmethoxyl)naphthalen- 2-ylmetho-xy]et hyl]benzoic acid, present considerable activity and improved pharmacokinetic profiles in comparison with our quinoline containing lead molecule confirming the interest of our compounds as potentially oral antiasthmatics and that the 4-alkylthiazole system can be considered as bioisosteric of the quinoline ring at least in our series of compounds.
机译:一组新的4- [2-(7-杂环甲氧基萘基-2-基甲氧基)乙基]苯甲酸已被合成,并在药理上被评价为LTD(4)-拮抗剂。与我们的含喹啉铅分子相比,噻唑衍生物,尤其是4- [2- [7-(4-环丁基噻唑-2-基甲氧基)萘--2-基甲基-xy] et羟基]苯甲酸具有相当大的活​​性并改善了药物动力学。证实了我们的化合物作为潜在的口服抗哮喘药的兴趣,并且至少在我们的一系列化合物中,4-烷基噻唑系统可以被认为是喹啉环的生物立体异构体。

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