Enguehard C, Renou J L, Allouchi H, Leger J M, Gueiffier A
Laboratoire de Chimie Thérapeutique, UFR des Sciences Pharmaceutiques, Tours, France,
Chem Pharm Bull (Tokyo). 2000 Jul;48(7):935-40. doi: 10.1248/cpb.48.935.
From a pharmacophore model of bicyclic heterocycles as aromatase inhibitors we have designed three series of imidazo[1,2-a]pyridine derivatives. The synthesis and the spectroscopy determination of various compounds are reported. The crystal data of one of these compounds (10b) was obtained. The aromatase inhibition potency was evaluated in vitro and no activity was found.
基于双环杂环作为芳香酶抑制剂的药效团模型,我们设计了三个系列的咪唑并[1,2-a]吡啶衍生物。报道了各种化合物的合成及光谱测定。获得了其中一种化合物(10b)的晶体数据。对芳香酶抑制活性进行了体外评估,未发现活性。