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.
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页数：6
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