Structure-activity relationships of anti-HIV-1 N-alkoxy- and N-allyloxy-benzimidazoles.
One-pot benzimidazole syntheses have been used to prepare an extended series of novel analogues which were evaluated against HIV-1 infectivity, the most active having an EC50 of 0.5pM. There is a correlation between the length of saturated alkyl groups at
Evans, Tahnee M.,Gardiner, John M.,Mahmood, Naheed,Smis, Marilyne
Efficient one-pot conversion of 6-methyl-2-nitroaniline into 1-alkyloxy-2-alkyl-4-methyl-, 1-benzyloxy-2-phenyl-4-methyl-, and 1-allyloxy-4-methyl-2-vinyl-benzimidazole
6-Methyl-2-nitroaniline reacts with alkyl, benzyl and allyl halides and NaH as base, to afford 1-alkoxy-2-alkyl-, 1-benzyloxy-2-aryl- and 1-allyloxy-2-vinyl-benzimidazoles in good to excellent yields (73-98%), via a novel one-pot N-alkylation-heterocycliz
Gardiner,Loyns
p. 819 - 827
(2007/10/02)
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