title: Synthesis and Anti-inflammatory Evaluation of Novel Benzimidazole and Imidazopyridine Derivatives.
abstract: Sepsis, an acute inflammatory disease, remains the most common cause of death in intensive care units. A series of benzimidazole and imidazopyridine derivatives were synthesized and screened for anti-inflammatory activities, and the imidazopyridine series showed excellent inhibition of the expression of inflammatory cytokines in LPS-stimulated macrophages. Compounds X10, X12, X13, X14, and X15 inhibited TNF-α and IL-6 release in a dose-dependent manner, and X12 showed no cytotoxicity in hepatic cells. Furthermore, X12 exhibited a significant protection against LPS-induced septic death in mouse models. Together, these data present a series of new imidazopyridines with potential therapeutic effects in acute inflammatory diseases.
authors.affiliation: School of Pharmacy, Wenzhou Medical College , 1210 University Town, Wenzhou, Zhejiang 325035, China.
authors.forename: Gaozhi
authors.initials: G
authors.lastname: Chen
authors.affiliation: School of Pharmacy, Wenzhou Medical College , 1210 University Town, Wenzhou, Zhejiang 325035, China.
authors.forename: Zhiguo
authors.initials: Z
authors.lastname: Liu
authors.affiliation: School of Environmental and Biological Engineering, Nanjing University of Science and Technology , 200 Xiaolingwei St., Nanjing, Jiangsu 210094, China.
authors.forename: Yali
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: Department of Pediatrics, The Second Affiliated Hospital, Wenzhou Medical College , Wenzhou, Zhejiang 325035, China.
authors.forename: Xiaoou
authors.initials: X
authors.lastname: Shan
authors.affiliation: Department of Pediatrics, The Second Affiliated Hospital, Wenzhou Medical College , Wenzhou, Zhejiang 325035, China.
authors.forename: Lili
authors.initials: L
authors.lastname: Jiang
authors.affiliation: School of Pharmacy, Wenzhou Medical College , 1210 University Town, Wenzhou, Zhejiang 325035, China.
authors.forename: Yunjie
authors.initials: Y
authors.lastname: Zhao
authors.affiliation: School of Pharmacy, Wenzhou Medical College , 1210 University Town, Wenzhou, Zhejiang 325035, China.
authors.forename: Wenfei
authors.initials: W
authors.lastname: He
authors.affiliation: School of Pharmacy, Wenzhou Medical College , 1210 University Town, Wenzhou, Zhejiang 325035, China.
authors.forename: Zhiguo
authors.initials: Z
authors.lastname: Feng
authors.affiliation: School of Environmental and Biological Engineering, Nanjing University of Science and Technology , 200 Xiaolingwei St., Nanjing, Jiangsu 210094, China.
authors.forename: Shulin
authors.initials: S
authors.lastname: Yang
authors.affiliation: School of Pharmacy, Wenzhou Medical College , 1210 University Town, Wenzhou, Zhejiang 325035, China.
authors.forename: Guang
authors.initials: G
authors.lastname: Liang
keywords: anti-inflammation; benzimidazoles; imidazopyridines; macrophages; sepsis