2. Academic Validation
  3. Synthesis of non-immunosuppressive cyclophilin-Binding cyclosporin A derivatives as potential anti-HIV-1 drugs

Synthesis of non-immunosuppressive cyclophilin-Binding cyclosporin A derivatives as potential anti-HIV-1 drugs

  • Bioorg Med Chem Lett. 2003 Dec 15;13(24):4415-9. doi: 10.1016/j.bmcl.2003.09.042.
Michel Evers 1,  Jean-Claude Barrière,  Georges Bashiardes,  Anne Bousseau,  Jean-Christophe Carry,  Norbert Dereu,  Bruno Filoche,  Yvette Henin,  Serge Sablé,  Marc Vuilhorgne,  Serge Mignani
Affiliations

Affiliation

  • 1 Aventis Pharma S.A., Centre de Recherche de Paris, 13 quai Jules Guesde, BP 14, 94403, Vitry-sur-Seine Cedex, France.
PMID: 14643337 DOI: 10.1016/j.bmcl.2003.09.042
Abstract

Original cyclosporin A (CsA) derivatives bearing various alkylthio side chains at the sarcosine residue 3 (R configuration) and for the most potent and selective compounds a 4'-hydroxyl group at the Me-Leucine residue 4 were prepared in one or two steps from commercially available CsA. The [2-(dimethyl or diethylamino)-ethylthio-Sar](3)-[(4'-OH)MeLeu](4)-CsA derivatives 3k and 3l displayed potent in vitro anti-HIV-1 (IC(50) approximately 46 nM) and low immunosuppressive activities (IC(50)>or=1500 nM).

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