Synthesis and Anti-HIV Activity of Cosalane Analogues with Substituted Benzoic Acid Rings Attached to the Pharmacophore through Methylene and Amide Linkers — Jeffrey A. Ruell (1999) | RDL Network
Synthesis and Anti-HIV Activity of Cosalane Analogues with Substituted Benzoic Acid Rings Attached to the Pharmacophore through Methylene and Amide Linkers
The cosalane pharmacophore has been extended by the attachment of two additional substituted benzoic acid rings through amide and methylene linkers. The resulting compounds display significant antiviral activity when tested in vitro for inhibition of the cytopathic effects of HIV-1RF in CEM-SS cells and HIV-1IIIB in MT-4 cells. The compound containing the methylene linker also shows moderate activity versus HIV-2ROD in MT-4 cells. Because cosalane and related compounds containing extended pharmacophores inhibit the binding of gp120 to CD4, the presently described new compounds are assumed to act by a similar mechanism. A hypothetical model is proposed for the binding of the methylene-linked compound to CD4.
K. C. Santhosh, Gitendra C. Paul, De Clercq Erik, Christophe Pannecouque, Myriam Witvrouw, Tracy L. Loftus, Jim A. Turpin, Robert W. Buckheit, Mark Cushman
Mark Cushman, Shabana Insaf, Gitendra C. Paul, Jeffrey A. Ruell, De Clercq Erik, Dominique Schols, Christophe Pannecouque, Myriam Witvrouw, Catherine A. Schaeffer, Jim A. Turpin, Karen Williamson, William G. Rice
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