作为抗病毒剂的咪唑并[1,2 - a]吡啶的合成。
Synthesis of imidazo[1,2-a]pyridines as antiviral agents.
作者信息
Gueiffier A, Mavel S, Lhassani M, Elhakmaoui A, Snoeck R, Andrei G, Chavignon O, Teulade J C, Witvrouw M, Balzarini J, De Clercq E, Chapat J P
机构信息
Laboratoire de Chimie Thérapeutique, Faculté de Pharmacie, Université de Tours, 31 Avenue Monge, 37200 Tours, France.
出版信息
J Med Chem. 1998 Dec 3;41(25):5108-12. doi: 10.1021/jm981051y.
The synthesis of original imidazo[1,2-a]pyridines bearing a thioether side chain at the 3 position and their antiviral activity are reported. From the synthesized compounds, 4, 15, and 21 were highly active against human cytomegalovirus with a therapeutic index superior to 150. These compounds also showed pronounced activity against varicella-zoster virus. Their structure-activity relationship is discussed.
报道了在3位带有硫醚侧链的新型咪唑并[1,2 - a]吡啶的合成及其抗病毒活性。在合成的化合物中，4、15和21对人巨细胞病毒具有高活性，治疗指数优于150。这些化合物对水痘 - 带状疱疹病毒也表现出显著活性。讨论了它们的构效关系。
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