title: [Synthesis of adenine derivatives and their activities against herpes virus in vitro].
abstract: A series of 9-(N4-substituted acetaldehyde thiosemicarbazone) adenines were synthesized and evaluated for antiherpes virus activity. Compounds 4a-l were prepared by condensation of 9-(acetaldehyde) adenine(6) and the corresponding N4-substituted thiosemicarbazides (10). The antiviral effects of all compounds 4a-l were tested in vitro in primary rabbit kidney cell cultures infected with herpes simplex virus type 1 (HSV-1) and varicella-herpes zoster virus (VZV), and in primary human embryo cell cultures infected with herpes simplex virus type 2 (HSV-2). The results showed that the minimum inhibitory concentrations (MIC) of 4e and 4f for HSV-1 and VZV were 20, 40, 20 and 20 micrograms.ml-1, respectively, and other compounds were 200 micrograms.ml-1. For HSV-2, the MIC of all tested compounds were 300 micrograms.ml-1. We also evaluated the antiherpetic effect of 4e (and 4f) by combination with acyclovir (ACV) in the ratio of 1:1 in vitro. The MIC of the combined compounds were 2 micrograms.ml-1 for 4e and 6 micrograms.ml-1 for 4f, while their minimum cytotoxicities (MCC) in the cell were markedly reduced compared with the individual compounds.
authors.affiliation: Faculty of Pharmacy, Shandong Medical University, Jinan.
authors.forename: M
authors.initials: M
authors.lastname: Zhong
authors.forename: Z P
authors.initials: ZP
authors.lastname: Liu
authors.forename: L J
authors.initials: LJ
authors.lastname: Xu
authors.forename: Z Y
authors.initials: ZY
authors.lastname: Wang
authors.forename: G T
authors.initials: GT
authors.lastname: Wang
mesh_terms: D000225:Adenine / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D018259:Herpesvirus 1, Human / Q000187:drug effects; D018258:Herpesvirus 2, Human / Q000187:drug effects; D014645:Herpesvirus 3, Human / Q000187:drug effects; D006801:Humans; D011817:Rabbits
chemical_list: D000998:Antiviral Agents; D000225:Adenine