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Synthesis and pharmacological activity of urea and thiourea derivatives of 4-azatricyclo[5.2.2.0(2,6)]undec-8-ene-3,5-dione
Authors:Struga Marta  Kossakowski Jerzy  Kedzierska Ewa  Fidecka Sylwia  Stefańska Joanna
Institution:Department of Medical Chemistry, The Medical University, 3 Oczki Str., 02-007 Warsaw, Poland. strugam@wp.pl
Abstract:A series of nineteen new thiourea and urea derivatives of 10-isopropyl-8-methyl-4-azatricyclo5.2.2.0(2,6)]undec-8-ene-3,5-dione, 1-isopropyl-7-methyl-4-azatricyclo5.2.2.0(2,6)]undec-8-ene-3,5-dione and 1,7,8,9,10-pentamethyl-4-azatricyclo5.2.1.0(2,6)]dec-8-ene-3,5-dione have been prepared and studied by (1)H-NMR. The compound k1a (1-(1,7,8,9,10-pentamethyl-3,5-dioxo-4-aza-tricyclo5.2.1.0(2,6)]dec-8-en-4-yl)-3-phenyl-urea) was tested for pharmacological activity on animal central nervous system (CNS). The activities of synthesized compounds were evaluated for their cytotoxicity and anti-HIV-1 activity in MT-4 cells. Antimicrobial activity of the newly obtained derivatives was tested against some Gram-positive and Gram-negative bacteria and fungi of the Candida species.
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