Synthesis and Anticoagulant Bioactivity of Heterocyclic Derivatives of Resveratrol
Twenty-five resveratrol derivatives were synthesized, among which eight compounds have not yet been reported. The target compounds were evaluated for thrombin inhibitory activity in vitro (IC50). The results showed that four compounds displayed a better thrombin inhibitory activity with IC50 values from 10.43 to 18.31 μM, better than resveratrol (25.87 μM). The R3 position of resveratrol was modified by heterocyclic rings containing oxygen and sulfur, which could increase the anticoagulant activity of resveratrol.
Keywordsresveratrol lipophilic derivatives heterocyclic rings anticoagulant activity thrombin
This work is financed by Shanghai College Students Innovative Projects (Nos. SH2016016 and SH2016018).
- 3.S. Bradamante, L. Barenghi, and A. Villa, Drug Rev., 22, 169 (2004).Google Scholar
- 18.Y. Lu, B. Yu, H. M. Dong, and T. Hong, Patent CN 102126993 (2011).Google Scholar
- 19.X. H. Chen, X. C. Dong, Z. F. Gao, and X. J. Sun, Chem. Reagents, 34, 6 (2012).Google Scholar