Synthesis and biological profiling of half-calycanthaceous alkaloid analogues

Abstract

During our continuous efforts to pursue antifungal agents, some calycanthaceous alkaloid analogs showed diverse and promising bioactivities. Therefore, 34 new calycanthaceous alkaloid derivatives were further prepared and screened for bioactivities. As a result of the evaluation against a great deal of plant pathogen fungi, bacteria and human pathogenic fungi, a majority of them displayed potent bioactivity. In particular, compound b6 displayed remarkably activity and might be novel potential leading compound for further development of antifungal agent. The relationship between structure and biological activity was also discussed.

Graphical abstract

Keywords:

• Calycanthaceous alkaloids
• synthesis
• plant pathogen fungi
• biological activity

Disclosure statement

The authors declare no conflict of interest.

Additional information

Funding

This work was financially supported by the National Natural Science Foundation of China (21502073), the Natural Science Foundation of Jiangsu Province (Grants No BK 20150465 and BK20180978), and the Key Research and Development Program (Modern Agriculture) of Zhenjiang City (NY2018002), Xinjiang Production Construction Corps Key Laboratory of Protection and Utilization of Biological Resources in Tarim Basin (BRYB1703), and Science and Technology Research Project of Shaanxi Province Academy of Sciences (2018nk-01), and Zhoushan Public Welfare Science and Technology Project (2019C31066).