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

doi:10.1039/C9CC07573A

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

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

*^ad

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* Corresponding authors

^a The State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300071, China
E-mail: 017095@nankai.edu.cn, lwang@nankai.edu.cn, yuechen@nankai.edu.cn

^b Accendatech Company, Ltd, Tianjin 300384, China

^c College of Pharmaceutical Sciences, Soochow University Medical College, Suzhou 215123, China

^d Collaborative Innovation Center of Chemical Sciences and Engineering, Tianjin, China

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.

Chemical Communications

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

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

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