Department of Chemistry, University of Victoria, Victoria, BC, Canada, V8W 3V6.
Org Lett. 2012 Dec 7;14(23):5876-9. doi: 10.1021/ol3027939. Epub 2012 Nov 26.
Rapid mutation of the influenza virus through genetic mixing raises the prospect of new strains that are both highly transmissible and highly lethal, and which have the ability to evade both immunization strategies (through mutation of hemagglutinin) and current therapies (through mutation of neuraminidase). Inspired by a need for next-generation therapeutics, a synthetic strategy for a new class of rigid, bicyclic inhibitors of influenza neuraminidase is reported.
流感病毒通过基因混合发生快速突变,增加了出现高传染性和高致死性新菌株的可能性,这些新菌株有能力逃避免疫策略(通过血凝素突变)和现有疗法(通过神经氨酸酶突变)。受开发下一代治疗方法的需求启发,报道了一种新型刚性双环流感神经氨酸酶抑制剂的合成策略。