Novel amidrazone derivatives: Design, synthesis and activity evaluation. Issue 12 (23rd July 2018)

• Record Type: Journal Article
• Authors: Zhou, Hua; Wang, Zhi Sen; Liu, Xin Hua; Chen, Fei Hu
• Is Part Of: Bioorganic & medicinal chemistry. Volume 26:Issue 12(2018)
• Page Start: 3158
• Page End: 3165
• Publication Date: 2018-07-23
• Subjects: ASIC activity -- Amidrazone -- Articular chondrocytes -- [Ca2+]i; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; Chemistry, Clinical -- Periodicals; Chemistry, Organic -- Periodicals; Chimie bio-organique -- Périodiques; Chimie pharmaceutique -- Périodiques; 615.19
• DOI: 10.1016/j.bmc.2018.04.042
• Languages: English
• ISSNs: 0968-0896

Abstract

Graphical abstract: Highlights: Novel naphthalenes as selectivity ASIC1a inhibitors were designed. Results revealed compound 5e showed activity to inhibit [Ca 2+ ]i . Compound 5e evaluated as potential ASIC1a inhibitor. Abstract: A series of new 6-styryl-naphthalene-2-amidrazone derivatives were synthesized and evaluated as potential ASIC1a inhibitors. Among them, compound 5e showed the most activity to inhibit [Ca 2+ ]i . elevation in acid-induced articular chondrocytes. Together with the important role of ASIC1a in the pathogenesis of tissue acidification diseases including rheumatoid arthritis, these results might provide a meaningful hint or inspiration in developing drugs targeting at tissue acidification diseases.