Synthesis and Pharmacological Activity of Urea and Thiourea Derivatives of 4-Azatricyclo[5.2.2.0^<2,6>]undec-8-ene-3,5-dione

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A series of nineteen new thiourea and urea derivatives of 10-isopropyl-8-methyl-4-azatricyclo[5.2.2.0^<2,6>]-undec-8-ene-3,5-dione, 1-isopropyl-7-methyl-4-azatricyclo[5.2.2.0^<2,6>]undec-8-ene-3,5-dione and 1,7,8,9,10-penta-methyl-4-azatricyclo[5.2.1.0^<2,6>]dec-8-ene-3,5-dione have been prepared and studied by ^1H-NMR. The compound k1a (1-(1,7,8,9,10-pentamethyl-3,5-dioxo-4-aza-tricyclo[5.2.1.0^<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.
公益社団法人日本薬学会の論文
2007-05-01