A series of new thiourea derivatives of 1,7,8,9-tetramethyl-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione have been prepared. The compound 6 was tested for pharmacological activity on animal central nervous system (CNS). The data suggest that compound 6 significantly interacts with 5-HT2 receptors in the brain. The activities of synthesized compounds were evaluated for their cytotoxicity and anti-HIV-1 activity in MT-4 cells. Elementary analysis, MS, 1H NMR spectra confirmed the identity of the products. The molecular structure of 12 was determined by an X-ray analysis.