82145-52-6Relevant academic research and scientific papers
Synthesis and Antiviral Activity of Novel N-Substituted Derivatives of Acyclovir
Boryski, Jerzy,Golankiewicz, Bozenna,Clercq, Erik De
, p. 1351 - 1355 (2007/10/02)
Novel N-substituted derivatives of acyclovir (1a) were synthesized and evaluated for their antiviral, antimetabolic, and antitumor cell properties in vitro.Monomethylation of 1a at positions 1, 7, and N-2 gave compounds 2-4, respectively.When positions 1 and N-2 were linked together by an isopreno group, the tricyclic 9--1,N-2-isopropenoquanine (5) was obtained.Compound 5 was then further methylated at positions N-2 and 7 to give 6 and 7, respectively.None of the new acyclovir derivatives showed any appreciable antimetabolic or antitumor cell activity.However, compounds 2 and 5 exhibited a marked antiherpetic activity.Their activity spectrum was similar to that of acyclovir, and their selectivity as inhibitors of herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2) was at least as great as, if not greater than, that of acylclovir.
N-alkylguanine acyclonucleosides as antiviral agents
-
, (2008/06/13)
Disclosed are compounds of the formula: STR1 and the pharmaceutically acceptable salts thereof wherein R1 and R2 are independently alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl or haloalkynyl, each having 1 to 19 carbon atoms, or R2 is hydrogen; R3 is hydrogen, alkyl having 1 to 6 carbon atoms or hydroxyalkyl having 1 to 6 carbon atoms; R4 is hydrogen, halogen, amino or alkyl having 1 to 4 carbon atoms; R5, R6 and R7 are independently selected from hydrogen, hydroxy, alkyl having 1 to 6 carbon atoms, acyloxy having 1 to 8 carbon atoms, alkoxy having 1 to 6 carbon atoms, hydroxyalkyl having 1 to 6 carbon atoms, acyloxyalkyl having 1 to 12 carbon atoms, amino, alkylamino of 1 to 6 carbon atoms and --PO3=, or two of R5, R6 and R7 taken together form a group --OPO2 O- --, --CH2 OPO2 O- --, --CH2 OPO2 OPO2 O= --, or --OPO2 OPO2 O= --; A is O, S or CH2 and X is a pharmaceutically acceptable anion. The compounds have antiviral activity, especially against viruses of the herpes class.
