title: Synthesis and anti-hepatitis B virus activity of some 2,3-dihydroxyprop-1-yl unnatural hetaryls.
abstract: The sodium salts of some hetaryls of the quinoxalin-2-ones 2-4, phthalazine-1,4-dione 5, phthalazin-1-one 6, and pyridazin-6-ones 7 and 8 were alkylated with (+/-) 2,3-O-isopropylidene-1-O-(4-toluenesulfonyl)glycerol (1) to give the respective tetraseco-nucleosides 9-15. Their deisopropylidenation with 70% acetic acid in water gave the corresponding 2,3-dihydroxyprop-1-yl hetaryls 16-22. Compounds 16-22 showed varying inhibition activity against Hepatitis B virus (HBV) with low to moderate cytotoxicity, where 18 and 21 showed the highest replication inhibition and low cytotoxicity.
authors.affiliation: Chemistry Department, Faculty of Science, Alexandria University, Egypt.
authors.lastname: el Ashry el-S
authors.forename: A A
authors.initials: AA
authors.lastname: Abdel-Rahman
authors.forename: N
authors.initials: N
authors.lastname: Rashed
authors.forename: H A
authors.initials: HA
authors.lastname: Rasheed
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002478:Cells, Cultured; D004279:DNA, Viral / Q000096:biosynthesis; D006515:Hepatitis B virus / Q000187:drug effects*; D006801:Humans; D016133:Polymerase Chain Reaction; D011409:Propylene Glycols / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000998:Antiviral Agents; D004279:DNA, Viral; D011409:Propylene Glycols