Synthesis and evaluation of inhibitory activity in vitro of dihydrostilbenes against human neutrophil elastases

Abstract

Twelve dihydrostilbenes (including five new analogues) were prepared by the Witting-Hornor reaction from appropriate aromatic aldehydes and phosphonate esters, followed by hydrogenation in five steps. The in vitro inhibition activity against human neutrophil elastase (HNE) of these dihydrostilbenes was evaluated, and three 1,2-dihydroxylated dihydrostilbenes (6b, 6j, and 6l) exhibited stronger inhibitory activity against HNE than other analogues.

Graphical Abstract

Keywords:

• Dihydrostilbenes
• synthesis
• human neutrophil elastase
• inhibition

Acknowledgments

The authors thank Prof. Yiming Li and Dr. Li Feng at Shanghai University of Traditional Chinese Medicine for providing HNE activity tests.

Disclosure statement

No potential conflict of interest was reported by the authors.

Funding

This investigation was financially supported by a grant (Nos 31260085 and 21861043) from the Natural Science Foundation of China, the Key Laboratory (No. 2016-5), and Science and Technology Innovation Team of Higher Education (No. 2014-6) in Yunnan, China.