European Journal of Medicinal Chemistry (2020)
Update date:2022-08-11
Topics:
Cao, Sheng
Cao, Yuting
Hou, Min
Jiang, Qiuyan
Li, Xiaohe
Lin, Gang
Liu, Xiang
Liu, Xinhua
Lu, Cheng
Mao, Jiahe
Peng, Junya
Qi, Min
Qin, Shuanglin
Song, Yang
Wei, Yujiao
Xie, Maodun
Yang, Cheng
Yang, Guang
Yang, Yuyu
Zhou, Honggang
Zhou, Yunyun
Idiopathic pulmonary fibrosis (IPF) and acute lung injury (ALI) are considered two severe public health issues, attributed to malfunctions of neutrophils. They can cause chronic inflammation and have association with subsequent tissue damages. There have been rare drugs applying to the efficient treatment in clinical practice. Existing research revealed that Leukotriene B4 (LTB4) is the critical endogenous molecule to induce neutrophil inflammatory response. LTB4 blocking biosynthesis is the potential strategy treating IPF and ALI. In the present study, 45 hydroxamic acid derivatives were produced, and compound 26 was screened out as a highly selective Lead compound of Leukotriene A4 Hydrolase (LTA4H), i.e., an enzyme critical to the biosynthesis of LTB4. This compound is capable of relieving neutrophilic inflammation in an IPF mouse model at early stage, as well as mitigating LPS-induced acute lung injury via a mechanism of LTB4 blocking biosynthesis in vivo. Whether this compound acts as the potential lead compound for the treatment of IPF and ALI requires further verification.
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