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
, 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

Nankai University
Accendatech Co., Ltd.
Soochow University
Collaborative Innovation Center of Chemical Science and Engineering

Research output: Contribution to journal › Article › peer-review

8 Citations (Scopus)

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 language	English
Pages (from-to)	11018-11021
Number of pages	4
Journal	Chemical Communications
Volume	56
Issue number	75
DOIs	https://doi.org/10.1039/c9cc07573a
Publication status	Published - 25 Sept 2020
Externally published	Yes

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10.1039/c9cc07573a

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title = "Chemical modification of ovatodiolide revealed a promising amino-prodrug with improved pharmacokinetic profile",

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.",

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

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doi = "10.1039/c9cc07573a",

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T1 - Chemical modification of ovatodiolide revealed a promising amino-prodrug with improved pharmacokinetic profile

AU - Xiang, Junhong

AU - Zhang, Xuemei

AU - Wang, Dehong

AU - Li, Jiaxin

AU - Li, Qiuying

AU - Wang, Qin

AU - Ding, Yahui

AU - Chen, Tianyang

AU - Sun, Yuanjun

AU - Bao, Shiqi

AU - Chen, Jing

AU - Li, Dongmei

AU - Wang, Liang

AU - Chen, Yue

PY - 2020/9/25

Y1 - 2020/9/25

N2 - 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.

AB - 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.

UR - https://www.scopus.com/pages/publications/85091469978

U2 - 10.1039/c9cc07573a

DO - 10.1039/c9cc07573a

M3 - Article

C2 - 32856652

AN - SCOPUS:85091469978

SN - 1359-7345

VL - 56

SP - 11018

EP - 11021

JO - Chemical Communications

JF - Chemical Communications

IS - 75

ER -

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

Abstract

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