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  • Joshi, Advait, et al. (author)
  • Design and Synthesis of P1-P3 Macrocyclic Tertiary-Alcohol-Comprising HIV-1 Protease Inhibitors
  • 2013
  • In: Journal of Medicinal Chemistry. - : American Chemical Society (ACS). - 0022-2623 .- 1520-4804. ; 56:22, s. 8999-9007
  • Journal article (peer-reviewed)abstract
    • To study P1-P3 macrocyclizations of previously reported tertiary-alcohol-comprising HIV-1 protease inhibitors (PIs), three new 14- and 15-member macrocyclic PIs were designed, synthesized by ring-closing metathesis, and evaluated alongside with 10 novel linear PIs. Cocrystallized complexes of the macrocyclic PIs and the HIV-1 protease are presented, analyzed, and discussed. The macrocyclic structures exhibited higher activities than the linear precursors with K-i and EC50 values down to 3.1 nM and 0.37 mu M, respectively.
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Type of publication
journal article (1)
Type of content
peer-reviewed (1)
Author/Editor
Larhed, Mats (1)
Hallberg, Anders (1)
Samuelsson, Bertil (1)
Wallberg, Hans (1)
Joshi, Advait (1)
Veron, Jean-Baptiste (1)
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Unge, Johan (1)
Rosenquist, Asa (1)
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University
Uppsala University (1)
Lund University (1)
Language
English (1)
Research subject (UKÄ/SCB)
Medical and Health Sciences (1)
Year
2013 (1)

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