Design and Synthesis of 4‐Alkyl‐2‐amino(acetamino)‐6‐aryl‐1, 3‐thiazine Derivatives as Influenza Neuraminidase Inhibitors. Issue 9 (7th August 2013)

• Record Type: Journal Article
• Authors: Li, Wan; Xia, Lin; Hu, Aixi; Liu, Ailin; Peng, Junmei; Tan, Weiqing
• Is Part Of: Archiv der Pharmazie. Volume 346:Issue 9(2013:Sep.)
• Page Start: 635
• Page End: 644
• Publication Date: 2013-08-07
• Subjects: Pharmaceutical chemistry -- Periodicals; Pharmacology -- Periodicals; 615.19
• DOI: 10.1002/ardp.201300122
• Languages: English
• ISSNs: 0365-6233

Abstract

<abstract abstract-type="main" xml:lang="en"> <title>Abstract</title> <sec id="ardp201300122-sec-0001" sec-type="section"> <p>With a convenient and economical method, two series of 1, 3‐thiazine derivatives <bold>1</bold> and <bold>2</bold> were synthesized, and their neuraminidase (NA) inhibitory activities were evaluated. The pharmacological results showed that most of the compounds have potent NA inhibitory activity. Especially, <bold>1g</bold> exhibited the best activity against influenza virus A (H1N1) NA (IC₅₀ = 29.06 µg/mL), and its crystal structure was determined by single‐crystal X‐ray diffraction. The preliminary biological assay indicated that 1, 3‐thiazine could be used as a core structure to design novel influenza NA inhibitors.</p> </sec> </abstract>