Design, synthesis, and bioactivity evaluation of novel 1-(4-(benzylsulfonyl)-2-nitrophenyl) derivatives as potential anti-inflammatory agents against LPS-induced acute lung injury

被引：0

作者：

Chen, Pan ^{[1
,2
,3
]}

Yu, Yiming ^{[1
]}

Su, Sijia ^{[1
]}

Du, Zhiteng ^{[1
]}

Cai, Binhao ^{[1
]}

Sun, Xiaoyu ^{[1
]}

Chattipakorn, Nipon ^{[5
]}

Samorodov, Aleksandr V. ^{[6
]}

Pavlov, Valentin N. ^{[6
]}

Tang, Qidong ^{[1
,3
]}

Cho, Won-Jea ^{[2
]}

Liang, Guang ^{[1
,3
,4
]}

机构：

[1] Wenzhou Med Univ, Chem Biol Res Ctr, Sch Pharmaceut Sci, Wenzhou 325035, Zhejiang, Peoples R China

[2] Chonnam Natl Univ, Coll Pharm, Gwangju 61186, South Korea

[3] Univ Chinese Acad Sci, Wenzhou Inst, Wenzhou 325001, Zhejiang, Peoples R China

[4] Hangzhou Med Coll, Sch Pharmaceut Sci, Hangzhou 311399, Zhejiang, Peoples R China

[5] Chiang Mai Univ, Fac Med, Cardiac Electrophysiol Res & Training Ctr, Chiang Mai 50200, Thailand

[6] Bashkir State Med Univ, Dept Pharmacol, Ufa 450005, Russia

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2023年 / 80卷

关键词：

Acute respiratory distress syndrome; Acute lung injury; Sulfur -containing compounds; Anti-inflammatory; INFLAMMATION;

D O I：

10.1016/j.bmcl.2022.129097

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Acute lung injury (ALI) is a devastating disease with a high mortality rate of 30%-40%. There is an unmet clinical need owing to limited treatment strategies and little clinical benefit. The pathology of ALI indicates that reducing the inflammatory response could be a highly desirable strategy to treat ALI. In this study, we designed and synthesized 36 novel 1-(4-(benzylsulfonyl)-2-nitrophenyl) derivatives and evaluated their anti-inflammatory activities by measuring the release of cytokines in lipopolysaccharide (LPS)-challenged J774A.1 cells. Com-pounds 19, 20, and 39 potently reduced the release of IL-6 and TNF-alpha in J774A.1 cells. Additionally, 39 improved LPS-induced ALI in vivo and inhibited cytokine production in lung tissues. Furthermore, 39 reduced inflammatory infiltration and downregulated p-p65 levels in lung tissues. Thus, compound 39 could serve as a new lead structure for the development of anti-inflammatory drugs to treat ALI.

引用

页数：6

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