1. Academic Validation
  2. Synthesis and anti-VZV activity of 6-heteroaryl derivatives of tricyclic acyclovir and 9-{[cis-1',2'-bis(hydroxymethyl)cycloprop-1'-yl]methyl}guanine analogues

Synthesis and anti-VZV activity of 6-heteroaryl derivatives of tricyclic acyclovir and 9-{[cis-1',2'-bis(hydroxymethyl)cycloprop-1'-yl]methyl}guanine analogues

  • Eur J Med Chem. 2009 Aug;44(8):3313-7. doi: 10.1016/j.ejmech.2009.03.005.
Tomasz Ostrowski 1 Bozenna Golankiewicz Erik De Clercq Graciela Andrei Robert Snoeck
Affiliations

Affiliation

  • 1 Institute of Bioorganic Chemistry, Polish Academy of Sciences, Poznan, Poland. tostr@ibch.poznan.pl
Abstract

A series of tricyclic analogues of acyclovir and 9-{[cis-1',2'-bis(hydroxymethyl)cycloprop-1'-yl]methyl}guanine substituted in the 6 position with thien-2-yl, 5-bromothien-2-yl or furan-2-yl group were synthesized. The new compounds 5a-f were evaluated for their activity in vitro against varicella-zoster virus (VZV) and cytomegalovirus (CMV). The marked anti-VZV activities of 5a-f remained comparable to those of their previously described 6-phenyl-substituted counterparts.

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