UDK: 615.3:547.854.4

OPTIMIZATION OF THE STRUCTURE OF METHYLATED 1-(BENZYLOXYMETHYL)-5-(ARYLAMINO) URACIL DERIVATIVES WITH ANTI-HIV-1 ACTIVITY

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

Волгоградский государственный медицинский университет, Научно-исследовательский институт фармакологии, ImQuestBioScience Inc. (США)

Abstract

New substituted derivatives of 1-(benzyloxymethyl)-5-(arylamino)uracil were synthesized by trimethylsilyl modification of Gilbert-Johnson method. The level of anti-HIV-1 activity of methylated 5-(benzylamino) derivatives depends on the site of methylation: 3,5-dimethylbenzylamino derivatives were found to be more active than corresponding - or N-methylated isomers.

Keywords

antiviral activity, HIV-1, uracil, pyrimidine.

Contacts

Озеров Александр Александрович — д. х. н., профессор, зав. кафедрой фармацевтической и токсикологической химии Волгоградского государственного медицинского университета, e-mail: prof_ozerov@yahoo.com