Tricyclic Aza-Andrographolide Derivatives from Late-Stage Hydroamination and Their Anti-human Coronavirus (Anti-HCoV) Activity

ACS Omega. 2022 Jul 7;7(28):24824-24837. doi: 10.1021/acsomega.2c02979. eCollection 2022 Jul 19.

ABSTRACT

A late-stage functionalization (LSF) of the natural product andrographolide for the efficient assembly of a range of structurally interesting and diverse tricyclic-aza derivatives was developed. The key to the diversification is a photo-catalyzed intramolecular hydroamination reaction, and acridinium derivatives were demonstrated to be the optimal catalysts. Additionally, the synthesized tricyclic aza-andrographolide derivatives were found to inhibit human coronavirus with high potency.

PMID:35874238 | PMC:PMC9301648 | DOI:10.1021/acsomega.2c02979

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