Journal
TETRAHEDRON
Volume 57, Issue 46, Pages 9385-9391Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0040-4020(01)00955-3
Keywords
cosalane; HIV; AIDS; gp120; CD4; bile acid; antiviral therapy
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Cosalane is a novel anti-HIV agent that inhibits the attachment of gp120 to CD4. The therapeutic potential of cosalane is limited by poor oral absorption. In an attempt to target the ileal bile acid transporter and thus facilitate oral bioavailability, a cosalane analog was synthesized in which the disalicylmethane pharmacophore is attached to a bile acid through a linker chain appended to C-17 of the steroid nucleus. The resulting bile acid analog of cosalane, retained antiviral activity vs. HIV-1(IIIB) and HIV-2(ROD) in MT-4 cells, but was less potent than cosalane. (C) 2001 Elsevier Science Ltd. All rights reserved.
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