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Design and Synthesis of P1-P3 Macrocyclic Tertiary-Alcohol-Comprising HIV-1 Protease Inhibitors

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Author

  • Advait Joshi
  • Jean-Baptiste Veron
  • Johan Unge
  • Asa Rosenquist
  • Hans Wallberg
  • Bertil Samuelsson
  • Anders Hallberg
  • Mats Larhed

Summary, in English

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.

Department/s

Publishing year

2013

Language

English

Pages

8999-9007

Publication/Series

Journal of Medicinal Chemistry

Volume

56

Issue

22

Document type

Journal article

Publisher

The American Chemical Society (ACS)

Topic

  • Medicinal Chemistry

Status

Published

ISBN/ISSN/Other

  • ISSN: 1520-4804