8-Aminobicyclo[3.2.1]octanes: synthesis and anti-viral activity

✍ Scribed by J.A Miller; G.M Ullah; G.M Welsh; A.C Hall

• Book ID: 104231642
• Publisher: Elsevier Science
• Year: 2001
• Tongue: French
• Weight: 165 KB
• Volume: 42
• Category: Article
• ISSN: 0040-4039
• DOI: 10.1016/s0040-4039(01)01593-3

✦ Synopsis

A series of 8-chlorobicyclo[3.2.1]oct-6-enes has been prepared from cyclohexenyl chlorides and simple alkynes via a one-step [3+2] cycloaddition methodology, and then converted into the corresponding bicyclic amines. Against influenza-A virus a number of these showed in vitro activity, and amine (2) was comparable to amantadine in vivo. Good activity against influenza-B virus was less common, and none of the amines showed high potency against both viruses. Amines ( 20) and ( 23) showed significant activity versus respiratory syncytial virus.