title: Synthesis and biological evaluation of N-substituted polycyclic imides derivatives.
abstract: The preparation of 16 derivatives of 3,5,8-trioxo-4-azatricyclo- [5.2.2.0(2.6)]undec-1-yl acetate and 8 derivatives of 1-isobutoxy-4-azatricyclo[5.2.2.0(2.6)]undecane-3,5,8-trione was described. Substituents to the imide N-atom were alkyl-(aryl)piperazine fragments with an alkyl linker being propyl or butyl group. Selected newly obtained compounds were evaluated in vitro against anti-HIV-1 activity. A broad group o fderivatives were tested for their antibacterial and antifungal activity. The pharmacological properties of butyl derivatives of imide 6 were evaluated in three behavioral tests in mice. The molecular structures of starting polycyclic 6-acetyl-imides, 1 and 5, were determined by X-ray crystallography. Presented tests have not revealed any activity of the compounds, however, selected derivatives exerted no neurotoxicity in behavioral tests.
authors.affiliation: Department of Medical Chemistry, The Medical University of Warsaw, 3 Oczki Street, 02-007 Warszawa, Poland. abielenica@wum.edu.pl
authors.forename: Anna
authors.initials: A
authors.lastname: Bielenica
authors.forename: Marta
authors.initials: M
authors.lastname: Struga
authors.forename: Barbara
authors.initials: B
authors.lastname: Mirosław
authors.forename: Anna E
authors.initials: AE
authors.lastname: Kozioł
authors.forename: Jerzy
authors.initials: J
authors.lastname: Kossakowski
authors.forename: Giuseppina
authors.initials: G
authors.lastname: Sanna
authors.forename: Paolo
authors.initials: P
authors.lastname: La Colla
authors.forename: Gabriele
authors.initials: G
authors.lastname: Giliberti
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000494:pharmacology; D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000935:Antifungal Agents / Q000494:pharmacology; D001522:Behavior, Animal / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D018360:Crystallography, X-Ray; D007094:Imides / Q000138:chemical synthesis* / Q000494:pharmacology*; D007202:Indicators and Reagents; D008297:Male; D051379:Mice; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D011083:Polycyclic Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D012044:Regression Analysis; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D019380:Anti-HIV Agents; D000935:Antifungal Agents; D007094:Imides; D007202:Indicators and Reagents; D011083:Polycyclic Compounds