通过生物等排酰胺取代发现强效和选择性双环 A(2B) 腺苷受体拮抗剂。
Discovery of potent and selective bicyclic A(2B) adenosine receptor antagonists via bioisosteric amide replacement.
机构信息
Almirall Research Center, Almirall S.A., Ctra. Laureà Miró 408, E-08980 St. Feliu de Llobregat, Barcelona, Spain.
出版信息
Bioorg Med Chem Lett. 2010 Mar 1;20(5):1634-7. doi: 10.1016/j.bmcl.2010.01.077. Epub 2010 Jan 20.
Several new potent and selective A(2B) adenosine receptor antagonists have been prepared in which the aryl-amide moiety of the lead series, exemplified by 1a, has been replaced by bioisosteric bicyclic moieties. Although the majority of compounds had generally improved microsomal stability as compared to 1a, this was not translated into overall improvements in the pharmacokinetic profiles of a representative set of compounds.
已经制备了几种新型强效和选择性 A(2B) 腺苷受体拮抗剂，其中以 1a 为代表的先导系列中的芳基酰胺部分已被生物等排双环部分取代。尽管与 1a 相比，大多数化合物通常具有更好的微粒体稳定性，但这并没有转化为一组代表性化合物的药代动力学特征的整体改善。
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