Véron Jean-Baptiste, Enguehard-Gueiffier Cécile, Snoeck Robert, Andrei Graciela, De Clercq Erik, Gueiffier Alain
Laboratoire de chimie thérapeutique, Faculté de pharmacie, EA 3857, 31 avenue Monge, 37200 Tours, France.
Bioorg Med Chem. 2007 Nov 15;15(22):7209-19. doi: 10.1016/j.bmc.2007.03.061. Epub 2007 Mar 24.
The synthesis of original imidazo[1,2-a]pyridines bearing a phenethylthiomethyl side chain at the 3 position and a (hetero)aryl substituent on the 6 or 8 position, and their antiviral activities are reported. From the synthesized compounds, the 6-halogeno and 6-phenylimidazo[1,2-a]pyridine derivatives 4c-d and 5b were the most potent against human cytomegalovirus (CMV) and/or varicella-zoster virus (VZV), whereas several other congeners (i.e., 5e, 5g, 5i, 5l, 5n, 5p, 5q, and 5t), while less potent, were equally or more selective in their inhibitory activity against both VZV and CMV. These compounds showed similar activity against thymidine kinase competent (TK(+)) and deficient (TK(-)) VZV strains, demonstrating a mechanism of action independent of the viral thymidine kinase.
报道了在3位带有苯乙硫基甲基侧链且在6或8位带有（杂）芳基取代基的新型咪唑并[1,2 - a]吡啶的合成及其抗病毒活性。在合成的化合物中，6 - 卤代和6 - 苯基咪唑并[1,2 - a]吡啶衍生物4c - d和5b对人巨细胞病毒（CMV）和/或水痘 - 带状疱疹病毒（VZV）最具活性，而其他几种同系物（即5e、5g、5i、5l、5n、5p、5q和5t）虽然活性较低，但对VZV和CMV的抑制活性具有同等或更高的选择性。这些化合物对胸苷激酶活性正常（TK(+)）和缺陷（TK(-)）的VZV菌株表现出相似的活性，证明其作用机制独立于病毒胸苷激酶。
