Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 56, Issue 22, Pages 8999-9007Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm400811d
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Funding
- Swedish Research Council (VR)
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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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