Article
Design, synthesis, evaluation, and crystallographic-based structural studies of HIV-1 protease inhibitors with reduced response to the V82A mutation.
Journal of medicinal chemistry - 28 Feb 2008
Clemente José C, Robbins Arthur, Graña Paula, Paleo M Rita, Correa Juan F, Villaverde M Carmen, Sardina F Javier, Govindasamy Lakshmanan, Agbandje-McKenna Mavis, McKenna Robert, Dunn Ben M, Sussman Fredy
Abstract excerpt
In our quest for HIV-1 protease inhibitors that are not affected by the V82A resistance mutation, we have synthesized and tested a second generation set of C2-symmetric HIV-1 protease inhibitors that contain a cyclohexane group at P1 and/or P1'. The binding affinity results indicate that these compounds have an improved response to the appearance of the V82A mutation than the parent compound. The X-ray structure...
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