SYNTHESIS AND EVALUATION OF NOVEL 6-(3,5-DIMETHYLBENZYL)URACIL ANALOGS AS POTENTIAL ANTI-HIV-1 AGENTS

© 2014 Nagy M. Khalifa^{a, b, #}, Erik B. Pedersen^c, Claus Nielsen^d, and Mohamed A. Al-Omar^a

^#E-mail: [email protected]

^aPharmaceutical Chemistry Department, Drug Exploration & Development Chair, College of Pharmacy, King Saud University, Riyadh 11451, Saudia Arabia;
^bTherapeutical Chemistry Department, Pharmaceutical and Drug Industries Division, National Research Centre, Dokki 12622, Cairo, Egypt;
^cDepartment of Chemistry, University of Southern Denmark, Dk;5230 Odense M, Denmark;
^dRetrovius Laboratory Department of Virology, State Serum Institute, DK;2300 Copenhagen, Denmark

Received December 28, 2013; in final form, January 31, 2014

A novel series of uracil derivatives with a 3,5-dimethylbenzyl group at the C-6 position were synthesized and evaluated as non-nucleoside HIV-1 reverse transcriptase inhibitors. Purity of the compounds has been confirmed by TLC. Structures of these compounds were established on the basis of elemental analyses and spectral studies. Some of the tested compounds showed moderate to potent activities against wild-type HIV-1, and N-1 alkylated derivatives were highly active.

Keywords: HIV-1 RT, S-DABOs analogues, HEPTs analogues, Anti HIV-1 activity

Биоорг. химия 2014, 40 (5): 629-635