Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44 West Wenhua Road, Jinan, Shandong 250012, China.
Bioorg Med Chem. 2011 Apr 1;19(7):2342-8. doi: 10.1016/j.bmc.2011.02.019. Epub 2011 Feb 17.
A series of thiazolidine-4-carboxylic acid derivatives were synthesized and evaluated for their ability to inhibit neuraminidase (NA) of influenza A virus. All the compounds were synthesized in good yields starting from commercially available l-cysteine hydrochloride using a suitable synthetic strategy. These compounds showed moderate inhibitory activity against influenza A neuraminidase. The most potent compound of this series is compound 4f (IC(50)=0.14 μM), which is about sevenfold less potent than oseltamivir and could be used to design novel influenza NA inhibitors that exhibit increased activity based on thiazolidine ring.
合成了一系列噻唑烷-4-羧酸衍生物，并评估了它们抑制甲型流感病毒神经氨酸酶（NA）的能力。所有化合物均以市售的盐酸 L-半胱氨酸为起始原料，采用合适的合成策略，以较高产率合成得到。这些化合物对甲型流感神经氨酸酶表现出中等抑制活性。该系列中最有效的化合物是化合物 4f（IC（50）=0.14 μM），其活性约为奥司他韦的七倍，可用于设计新型基于噻唑烷环的流感 NA 抑制剂，以提高其活性。
