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AssigneeChina Pharmaceutical University
InventorsQidong You, Zhengyu Jiang, Mengchen Lu, Xian Zhang, Jing Zhao, Xiaoke Guo, Xiaoli Xu, Lei Wang
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The present application relates to a hydrogen peroxide-responsive Keap1-Nrf2 PPI inhibitor prodrug, and a preparation method therefor. The hydrogen peroxide-responsive Keap1-Nrf2 PPI inhibitor prodrug pro2 has a chemical structure as shown below. By modifying a key carboxyl pharmacophore in a Keap1-Nrf2 inhibitor with a H2O2-responsive thiazolidinone moiety, a novel ROS-responsive antioxidant prodrug pro2 is synthesized. The H2O2 activated prodrug pro2 can simultaneously achieve targeted activation of Nrf2 and enhancement of therapeutic efficacy in the body. The prodrug is based on the concept of ROS activation-ROS clearance therapy, is the first example of a H2O2-responsive prodrug suitable for oral administration, and is expected to be used clinically by virtue of the characteristics of druggability and high targeting ability.
A prodrug pro2 of hydrogen peroxide-responsive Keap1-Nrf2 PPI inhibitor having the following structural formula:
A method for preparing a prodrug pro2, wherein a synthetic route is as follows:
A method for preparing a prodrug pro2 in preparing an anti-inflammatory drug, the prodrug pro2 having the following structural formula:
Dependencies are inferred from the claim text.