Imidazopyridine-5,6,7,8-tetrahydro-8-quinolinamine derivatives with potent activity against HIV-1.
Synthesis of several novel imidazopyridine-5,6,7,8-tetrahydro-8-quinolinamine derivatives with potent activity against HIV are described. Synthetic approaches allowing for variation of the substitution pattern are outlined and resulting changes in antiviral activity and pharmacokinetics are highlighted. Several compounds with low nanomolar anti-HIV activity and oral bioavailability are described.
Gudmundsson
Kristjan S
KS
Department of Medicinal Chemistry, Metabolic and Virology Center of Excellence for Drug Discovery, GlaxoSmithKline Research & Development, Five Moore Drive, Research Triangle Park, NC 27709-3398, USA. ksgudmundsson@gmail.com
Boggs
Sharon D
SD
Catalano
John G
JG
Svolto
Angilique
A
Spaltenstein
Andrew
A
Thomson
Michael
M
Wheelan
Pat
P
Jenkinson
Stephen
S
D019380:Anti-HIV Agents / Q000493:pharmacokinetics / Q000627:therapeutic use; D000998:Antiviral Agents / Q000494:pharmacology / Q000627:therapeutic use*; D045744:Cell Line, Tumor; D006678:HIV / Q000737:chemistry; D015658:HIV Infections / Q000188:drug therapy; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D008956:Models, Chemical
D019380:Anti-HIV Agents; D000998:Antiviral Agents