title: Identification of antibacterial and antiviral activities of novel fused 1,2,4-triazine esters.
abstract: The in vitro biological activities of novel derivatives of methyl and ethyl 2-(4-oxo-8-aryl-2H-3,4,6,7-tetrahydroimidazo[2,1-c][1,2,4]triazin-3-yl)acetates (3a, 3d-j) have been evaluated and are reported. The final heterobicycles (3a-j) were obtained from monocyclic 1-aryl-2-hydrazonoimidazolidines (2a-f) by addition and cyclization reaction with fumaric acid esters. In particular, compounds 3d and 3e were found to exhibit comparable antibacterial potencies in vitro as that of ampicillin. Heterobicycles of the 3e, 3g and 3j type were screened for their antiviral activities against the selected viruses' DNA (human adenovirus type 5-Ad-5) and RNA (human enterovirus-Echo-9). Simultaneously, their cytotoxicities towards HEK-293 and GMK cells were established. In particular, heterobicycle 3j, completely non-toxic for GMK cells, was found to exhibit virucidal properties against Echo-9 virus justifying its further investigation as the potential antiviral agent.
authors.affiliation: Department of Medical Chemistry, Professor Feliks Skubiszewski Medical University, 4 Staszica Street, 20-081 Lublin, Poland. kryzysztof.sztanke@am.lublin.pl
authors.forename: Krzysztof
authors.initials: K
authors.lastname: Sztanke
authors.forename: Kazimierz
authors.initials: K
authors.lastname: Pasternak
authors.forename: Barbara
authors.initials: B
authors.lastname: Rajtar
authors.forename: Małgorzata
authors.initials: M
authors.lastname: Sztanke
authors.forename: Magdalena
authors.initials: M
authors.lastname: Majek
authors.forename: Małgorzata
authors.initials: M
authors.lastname: Polz-Dacewicz
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity*; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity*; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D004952:Esters / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity*; D006571:Heterocyclic Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000633:toxicity; D006801:Humans; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D014227:Triazines / Q000737:chemistry*
chemical_list: D000900:Anti-Bacterial Agents; D000998:Antiviral Agents; D004952:Esters; D006571:Heterocyclic Compounds; D014227:Triazines