Chemical modification of ovatodiolide revealed a promising amino-prodrug with improved pharmacokinetic profile

Junhong Xiang, Xuemei Zhang, Dehong Wang, Jiaxin Li, Qiuying Li, Qin Wang, Yahui Ding*, Tianyang Chen, Yuanjun Sun, Shiqi Bao, Jing Chen, Dongmei Li, Liang Wang, Yue Chen

*Corresponding author for this work

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Abstract

Stepwise modification of ovatodiolide revealed a prodrug, NMP-diepoxyovatodiolide, which can provide sustained release of an active compound, substantial metabolic stability and a unique accumulation profile in the liver. Besides, NMP-diepoxyovatodiolide demonstrated therapeutic benefits in an acute autoimmune hepatitis mouse model and a broad safety window. Therefore, NMP-diepoxyovatodiolide is a very promising candidate for further development of liver-related drugs.

Original languageEnglish
Pages (from-to)11018-11021
Number of pages4
JournalChemical Communications
Volume56
Issue number75
DOIs
Publication statusPublished - 25 Sept 2020
Externally publishedYes

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Xiang, J., Zhang, X., Wang, D., Li, J., Li, Q., Wang, Q., Ding, Y., Chen, T., Sun, Y., Bao, S., Chen, J., Li, D., Wang, L., & Chen, Y. (2020). Chemical modification of ovatodiolide revealed a promising amino-prodrug with improved pharmacokinetic profile. Chemical Communications, 56(75), 11018-11021. https://doi.org/10.1039/c9cc07573a