Design, synthesis and anti-HIV activity of homologous PMEA derivatives.
This article describes an efficient route for synthesizing novel cyclopropyl homologous PMEA analogues. The condensation of the bromide 8 with nucleosidic bases (A, U, T, C, 5-FU, G) under standard nucleophilic substitution and deprotection conditions, afforded the target phosphonic acid analogues 14 approximately 18 and 21. These compounds were evaluated for their potential antiviral properties against various viruses. Guanine derivative 21 showed significant antiviral activity.
Oh
Chang Hyun
CH
Medicinal Chemistry Research Center, Korea Institute of Science and Technology, Seoul, Republic of Korea.
Hong
Joon Hee
JH
D000225:Adenine / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology / Q000031:analogs & derivatives; D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D015658:HIV Infections / Q000188:drug therapy; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans
C120290:9-(2-(phosphonomethoxy)ethyl)adenine diphosphate; D019380:Anti-HIV Agents; D000225:Adenine