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  • Design, synthesis and biological activity of thiazolidine-4-carboxylic acid derivatives as novel influenza neuraminidase inhibitors.

Design, synthesis and biological activity of thiazolidine-4-carboxylic acid derivatives as novel influenza neuraminidase inhibitors.

Bioorganic & medicinal chemistry (2011-03-09)
Yu Liu, Fanbo Jing, Yingying Xu, Yuanchao Xie, Fangyuan Shi, Hao Fang, Minyong Li, Wenfang Xu
ABSTRACT

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.

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Sigma-Aldrich
L-4-Thiazolidinecarboxylic acid, 98%
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1 g
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CN¥2,480.33