Structure-based design of diaminopyranosides as a novel inhibitor core unit of HIV proteases.
Novel HIV PR inhibitors, which contain a diaminopyranoside moiety as an inhibitor core unit, were designed based on the 3D structures of complexes of HIV-1 PR with transition-state mimics. These compounds were examined for their ability to inhibit the hydrolytic activity of a recombinant HIV-1 PR.
D000599:Amino Acids, Diamino / Q000138:chemical synthesis* / Q000737:chemistry* / Q000493:pharmacokinetics*; D015195:Drug Design; D017320:HIV Protease Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry* / Q000493:pharmacokinetics*; D008956:Models, Chemical