Design and Synthesis of Cinanserin Analogs as Severe Acute Respiratory Syndrome Coronavirus 3CL Protease Inhibitors

Qingang Yang; Lili Chen; Xuchang He; Zhenting Gao; Xu Shen; Donglu Bai

doi:10.1248/cpb.56.1400

Regular Articles

Design and Synthesis of Cinanserin Analogs as Severe Acute Respiratory Syndrome Coronavirus 3CL Protease Inhibitors

Qingang Yang, Lili Chen, Xuchang He, Zhenting Gao, Xu Shen, Donglu Bai

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Keywords: SARS coronavirus 3CL protease, cinanserin analog, inhibitor, fluorescence resonance energy transfer-based assay

JOURNAL FREE ACCESS

2008 Volume 56 Issue 10 Pages 1400-1405

DOI https://doi.org/10.1248/cpb.56.1400

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Abstract

The severe acute respiratory syndrome (SARS) coronavirus 3CL protease is an attractive target for the development of anti-SARS drugs. In this paper, cinanserin (1) analogs were synthesized and tested for the inhibitory activities against SARS-coronavirus (CoV) 3CL protease by fluorescence resonance energy transfer (FRET) assay. Four analogs show significant activities, especially compound 26 with an IC₅₀ of 1.06 μM.

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