Allen Scott H, Johns Brian A, Gudmundsson Kristjan S, Freeman George A, Boyd F Leslie, Sexton Connie H, Selleseth Dean W, Creech Katrina L, Moniri Kelly R
Department of Medicinal Chemistry, GlaxoSmithKline Research and Development, Research Triangle Park, NC 27709, USA.
Bioorg Med Chem. 2006 Feb 15;14(4):944-54. doi: 10.1016/j.bmc.2005.09.015. Epub 2005 Oct 4.
A novel series of potent C-6 substituted pyrazolo[1,5-a]pyridine inhibitors of herpes simplex viruses has been identified. A synthetic methodology was developed involving functionalization of a C-6 trifluoromethyl pyrazolo[1,5-a]pyridine to allow facile access to a diverse set of analogues from common late stage intermediates. The expansion of the SAR of this series at the 6 position allows for modifications to developability parameters such as clogP, while maintaining potency comparable to acyclovir.
已鉴定出一系列新型的强效C-6取代的吡唑并[1,5-a]吡啶单纯疱疹病毒抑制剂。开发了一种合成方法，该方法涉及对C-6三氟甲基吡唑并[1,5-a]吡啶进行官能化，以便从常见的后期中间体轻松获得各种类似物。该系列在6位的构效关系扩展允许对诸如clogP等可开发性参数进行修饰，同时保持与阿昔洛韦相当的效力。
