UDK: 615.3: 547.854.4

Novel n-[2-(benzoylphenoxy)ethyl] nucleic bases deriv atives - synthesis and anti-hiv-1 activity in vitro

A. A. Ozerov, M. S. Novikov, A. I. Luganchenko, T. Hartman, R. W. Buckheit

Волгоградский государственный медицинский университет, кафедра фармацевтической и токсикологической химии, ImQuest BioSciences, Inc., Maryland, USA

Abstract

New benzophenone derivatives of pyrimidine nucleic bases have been synthesized by alkylation of the ir trimethylsilyl derivatives with isomeric 1-bromo-2-(benzoylphenoxy)ethanes. Ortho-derivatives of uracil and thymine demonstrated a high antiviral activity in vitro with EC 50 value of 0,030 and 0,009 µM, respectively. Meta- and para-isomers were totally inactive.

Keywords

anti-HIV-1 activity, pyrimidine, benzophenone

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