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BACKGROUND Following the example of L-valine prodrugs of antiviral nucleoside analogues, L-valine ester of cyclopropavir (valcyclopropavir) was synthesized. METHODS The known tetrahydropyranylcyclopropavir was transformed to N-(tert-butoxycarbonyl)-L-valine ester, which was deprotected to valcyclopropavir. RESULTS Stability of valcyclopropavir towards hydrolysis at pH 7.0 roughly corresponded to that of valganciclovir. Valcyclopropavir inhibited replication of human cytomegalovirus (HCMV, Towne and AD169 strains) to approximately the same extent as the parent drug cyclopropavir. Pharmacokinetic studies in mice established that the oral bioavailability of valcyclopropavir was 95%. CONCLUSIONS The prodrug valcyclopropavir offers some improved therapeutic parameters over the parent compound cyclopropavir.
Zhimeng Wu, and
John C Drach, and
Mark N Prichard, and
Milka Yanachkova, and
Ivan Yanachkov, and
Terry L Bowlin, and
Jiri Zemlicka
April 2012,
Bioorganic & medicinal chemistry,
Zhimeng Wu, and
John C Drach, and
Mark N Prichard, and
Milka Yanachkova, and
Ivan Yanachkov, and
Terry L Bowlin, and
Jiri Zemlicka
January 1969,
Tetrahedron letters,
Zhimeng Wu, and
John C Drach, and
Mark N Prichard, and
Milka Yanachkova, and
Ivan Yanachkov, and
Terry L Bowlin, and
Jiri Zemlicka
August 1963,
Experientia,
Zhimeng Wu, and
John C Drach, and
Mark N Prichard, and
Milka Yanachkova, and
Ivan Yanachkov, and
Terry L Bowlin, and
Jiri Zemlicka
June 2021,
Materials (Basel, Switzerland),
Zhimeng Wu, and
John C Drach, and
Mark N Prichard, and
Milka Yanachkova, and
Ivan Yanachkov, and
Terry L Bowlin, and
Jiri Zemlicka
March 2003,
Inorganic chemistry,
Zhimeng Wu, and
John C Drach, and
Mark N Prichard, and
Milka Yanachkova, and
Ivan Yanachkov, and
Terry L Bowlin, and
Jiri Zemlicka
May 2012,
Biomolecules & therapeutics,
Zhimeng Wu, and
John C Drach, and
Mark N Prichard, and
Milka Yanachkova, and
Ivan Yanachkov, and
Terry L Bowlin, and
Jiri Zemlicka
November 2014,
International journal of pharmaceutics,
Zhimeng Wu, and
John C Drach, and
Mark N Prichard, and
Milka Yanachkova, and
Ivan Yanachkov, and
Terry L Bowlin, and
Jiri Zemlicka
October 2011,
Molecular pharmaceutics,
Zhimeng Wu, and
John C Drach, and
Mark N Prichard, and
Milka Yanachkova, and
Ivan Yanachkov, and
Terry L Bowlin, and
Jiri Zemlicka
January 2012,
Antimicrobial agents and chemotherapy,
Zhimeng Wu, and
John C Drach, and
Mark N Prichard, and
Milka Yanachkova, and
Ivan Yanachkov, and
Terry L Bowlin, and
Jiri Zemlicka
December 1982,
Journal of pharmacokinetics and biopharmaceutics,
