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Alkylation of 2-methylthiopyrimidin-4(1H)-one (1a) and its 5(6)-alkyl derivatives 1b-d as well as theophylline (7) with 2,2-bis(bromomethyl)-1,3-diacetoxypropane (2) under microwave irradiation gave the corresponding acyclonucleosides 1-[(3-acetoxy-2-acetoxymethyl-2-bromomethyl)prop-1-yl]-2-methyl-thio pyrmidin-4(1H)-ones 3a-d and 7-[(3-acetoxy-2-acetoxymethyl-2-bromomethyl)prop-1-yl]theophylline (8), which upon further irradiation gave the double-headed acyclonucleosides 1,1 '-[(2,2-diacetoxymethyl)-1,3-propylidene]-bis[(2-(methylthio)-pyrimidin-4(1H)-ones] 4a-c, and 7,7 '-[(2,2-diacetoxymethyl)-1,3-propylidene]-bis(theophylline) (9). The deacetylated derivatives were obtained by the action of sodium methoxide. The activity of deacetylated nucleosides against Hepatitis B virus was evaluated. Compound 5b showed moderate inhibition activity against HBV with mild cytotoxicity.

Homoacyclovir Analogues of Unnatural Bases and Their Activity Against Hepatitis B Virus. -Seven compounds of type (V) are tested for their activities against hepatitis B virus. Three of them, viz. (V), show high inhibition activity and low cytotoxicity. -(EL ASHRY, E. S. H.; ABDEL-RAHMAN, A. A.-H.; RASHED, N.; RASHEED, H. A.; Pharmazie 54 (1999) 12, 893-897; Dep. Chem., Fac. Sci., Alexandria Univ., Alexandria 21321, Egypt; EN)

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.