Polysulfated sialic acid derivatives as anti-human immunodeficiency virus

We report the synthesis of a novel alkyl polysulfated sialic acid derivative denoted as NMSO,. NMSO, exhibited potent inhibition against both laboratory and clinical human immunodeficiency virus type 1 (HIV-1). The anti-viral activity of this compound (I uM) was compared to dextran sulfate (3 uM), and was found to be more potent against HIV-1(IIIb) than AZT (10 uM). The anti-coagulation time was more than 15-fold shorter than that of dextran sulfate. An in vivo anti-viral study of NMSO, in NOD-SCID-PBL mice HIV model showed complete protection of the animals from virus challenge at the concentration of 10 mg/kg. This suggests that NMSO3 can be effective in the treatment of HIV-infected individuals. (c) 2005 Elsevier SAS. All rights reserved.